GPCR/G-Protéine
Les inhibiteurs des GPCR/protéines G sont des composés qui ciblent les récepteurs couplés aux protéines G (GPCR) et les protéines G associées, qui jouent un rôle crucial dans la transmission des signaux de l'extérieur vers l'intérieur des cellules. Ces inhibiteurs sont essentiels pour étudier les voies de signalisation médiées par les GPCR, impliquées dans de nombreux processus physiologiques, y compris la perception sensorielle, la réponse immunitaire et la neurotransmission. Les inhibiteurs des GPCR sont également importants dans le développement de médicaments, car de nombreux agents thérapeutiques ciblent ces récepteurs. Chez CymitQuimica, nous offrons une large gamme d'inhibiteurs de GPCR/protéines G de haute qualité pour soutenir vos recherches en pharmacologie, biologie cellulaire et domaines connexes.
Sous-catégories appartenant à la catégorie "GPCR/G-Protéine"
- récepteur 5-HT(1.025 produits)
- Récepteur d'adénosine(249 produits)
- Récepteur adrénergique(3.024 produits)
- Récepteur de la bombésine(35 produits)
- Récepteur de la bradykinine(61 produits)
- CXCR(158 produits)
- CaSR(34 produits)
- Récepteur cannabinoïde(217 produits)
- Cholécystokinine(1 produits)
- Récepteur de la dopamine(445 produits)
- Récepteur de l'endothéline(86 produits)
- Récepteur GNRH(84 produits)
- GPCR19(33 produits)
- GRK(33 produits)
- GTPase(23 produits)
- Récepteur du glucagon(194 produits)
- Hérisson/Smoothened(49 produits)
- Récepteur de l'histamine(385 produits)
- Récepteur LPA(21 produits)
- Récepteur de la mélatonine(26 produits)
- Récepteur OX(41 produits)
- Récepteur opioïde(327 produits)
- PAFR(14 produits)
- PKA(60 produits)
- Récepteur S1P(18 produits)
- SGLT(31 produits)
- Récepteur Sigma(46 produits)
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5990 produits trouvés pour "GPCR/G-Protéine"
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CP-199330
CAS :CP-199330: non-toxic alternative to Zafirlukast & Pranlukast, blocks cysteyl LT1 receptors.Formule :C28H24ClF3N2O6SCouleur et forme :SolidMasse moléculaire :609.01(S)-YNT-3708
CAS :(S)-YNT-3708 is the S-isomer of YNT-3708, demonstrating relatively low activity against OX1R and OX2R receptors, with EC50 values of 3595 nM and 1661 nM, respectively.Formule :C35H36N4O6SCouleur et forme :SolidMasse moléculaire :640.749L-654284
CAS :L-654284 is an α2-adrenergic receptor antagonist characterized by its notable selectivity. It competes with 3H-clonidine and 3H-rauwolscine for binding in vitro, exhibiting Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 effectively blocks the pre-ejaculatory effects of clonidine in isolated rat vas deferens, with a pA2 value of 9.1. The compound demonstrates significant selectivity for α2 over α1 adrenergic receptors, with a Ki value of 110 nM against 3H-prazosin binding. In vivo, L-654284 significantly increases the turnover of norepinephrine in the rat cerebral cortex, indicating its activity in blocking α2-adrenergic receptors within the central nervous system.Formule :C18H24N2O4SCouleur et forme :SolidMasse moléculaire :364.46Hoe 892
CAS :Hoe 892 is a stable thia-thimo-analogue of prostacyclin and acts as a platelet aggregation inhibitor.Formule :C20H33NO4SCouleur et forme :SolidMasse moléculaire :383.5516(R)-Iloprost
CAS :Iloprost, a potent prostacyclin analog, binds IP & EP1 receptors (Ki 11 nM), contains 16(S/R) isomers, and inhibits platelets (IC50 65 nM).Formule :C22H32O4Couleur et forme :SolidMasse moléculaire :360.49CB2 receptor antagonist 1
CAS :Compound 29 is a potent, CB2-selective antagonist/reverse agonist. Derivatives 23 & 24 offer antinociception; 24 activates cannabinoid/TRPV1 receptors.Formule :C28H47NO3Couleur et forme :SolidMasse moléculaire :445.68RU 52583
CAS :RU 52583 is an alpha 2-adrenergic receptor antagonist.Formule :C18H20N2Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :264.36KARI 201 hydrochloride
CAS :KARI 201 hydrochloride is a selective, brain-penetrant, competitive inhibitor of acid sphingomyelinase (ASM) with an IC50 of 338.3 nM. It also acts as an agonist for the growth hormone-releasing peptide receptor (ghrelin receptor). Additionally, KARI 201 hydrochloride can enhance the neuropathological features of Alzheimer's disease.Formule :C14H29ClN4O2Couleur et forme :SolidMasse moléculaire :320.86DSP-1053 benzenesulfonate
CAS :DSP-1053: Benzylpiperidine-based, potent SERT inhibitor (Ki=1.02nM), partial 5-HT1A receptor agonist (Ki=5.05nM), antidepressant.Formule :C32H38BrNO7SCouleur et forme :SolidMasse moléculaire :660.62Pareptide monohydrochloride
CAS :Pareptide monohydrochloride is a metabolically stable analog of melatonin inhibitor (MIF).Formule :C14H27ClN4O3Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :334.84MRT-92
CAS :MRT-92 is an antagonist of Smoothened (Smo) with anti-cancer activity, featuring a binding affinity (Ki) of 0.7 nM. It inhibits the Hedgehog signaling pathway by obstructing the overlapping binding sites within the transmembrane domain of the Smoothened receptor and suppresses the proliferation of cerebellar granule cells in rodents (IC50=0.4 nM). MRT-92 is utilized for research into cerebellar gliomas.Formule :C33H34N4O5Couleur et forme :SolidMasse moléculaire :566.65Rocavorexant
CAS :Rocavorexant is an antagonist of the orexin-1 receptor (orexin-1 receptor), exhibiting a pIC50 value of 9.1 for human OX1 and a pIC50 of 6.0 for human OX2.Formule :C18H19F3N8OCouleur et forme :SolidMasse moléculaire :420.392(+)-15-epi Cloprostenol
CAS :(+)-15-epi Cloprostenol is a synthetic analogue of prostaglandin F2α (PGF2α) and functions as a potent FP receptor agonist. The compound (+)-15-epi Cloprostenol is the 15(S) or 15β-hydroxy enantiomer of (+)-(+)-15-epi Cloprostenol. Compared to the 15(R)-(+)-15-epi Cloprostenol, this epimer exhibits significantly lower activity as an FP receptor ligand. However, the specific activity of this isomer remains inadequately studied.Formule :C22H29ClO6Masse moléculaire :424.92Org-6906
CAS :DCB-3503, a tylophorine analog, may treat cancer and suppress immunity by blocking protein synthesis and modulating HSC70's ATPase activity.Formule :C13H16ClNDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :221.73RS 12254
CAS :RS 12254 is a dopamine agonist and antihypertensive agent.Formule :C28H40N2O4Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :468.63LRH-1 modulator-1
CAS :LRH-1 modulator-1: potent agonist, boosts IL-10, reduces IL-1b/TNFa, anti-inflammatory in gut.Formule :C28H36N2O2SCouleur et forme :SolidMasse moléculaire :464.66GnRH-R antagonist 1
CAS :Compound 21a: Oral GnRH-R antagonist, IC50=0.57 nM, potent against prostate cancer/prevents LH surges.Formule :C31H28F5N7O6SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :721.65GLP-1 receptor agonist 10
CAS :GLP-1 Receptor Agonist 10 (Compound 42), an agonist of the GLP receptor, reduces glucose excursions and inhibits food intake in mice. It is useful for research into type 2 diabetes (T2DM) and obesity [1].Formule :C30H28F4N6O5Couleur et forme :SolidMasse moléculaire :628.57LPA5 antagonist 3
CAS :LPA5 antagonist 3 (Example 74), a lysophosphatidic acid receptor 5 (LPA5) antagonist, exhibits potent activity with an IC50 value of 170 nM. It is primarily utilized in the research of pain disorders and atherosclerosis [1].Formule :C24H20F3NO4Masse moléculaire :443.42BIIE-0246 HCl
CAS :BIIE-0246: A potent, non-peptide Y2 receptor antagonist; >650-fold more selective than Y1, Y4, Y5.Formule :C49H59Cl2N11O6Couleur et forme :SolidMasse moléculaire :968.97JKC 302
CAS :JKC 302 is an ET-A receptor antagonist that partially inhibits the contraction of tracheal rings in asthmatic rats induced by ET-1.Formule :C30H42N6O6Couleur et forme :SolidMasse moléculaire :582.69AL 8810
CAS :AL-8810 is an 11β-fluoro analog of PGF 2α with selective antagonist effects at the PGF 2α receptor (FP receptor) [1].Formule :C24H31FO4Couleur et forme :SolidMasse moléculaire :402.52,3-MDMA hydrochloride
CAS :2,3-MDMA hydrochloride is an inhibitor of the noradrenalin transporter and serotonin transporter, with IC50 values of 6.2 μM and 82 μM, respectively.Formule :C11H16ClNO2Couleur et forme :SolidMasse moléculaire :229.703AM11638
CAS :AM11638 is an endogenous cannabinoid analogue that targets cannabinoid receptors (CB1 and CB2 receptors), exhibiting analgesic properties. It shows potential for research in neurological disorders and inflammation-related diseases.Formule :C27H41NO2Couleur et forme :SolidMasse moléculaire :411.62CCR1 antagonist 13
CAS :CCR1 antagonist13 is a selective small molecule antagonist of CCR1.Formule :C25H27ClFN3O4Couleur et forme :SolidMasse moléculaire :487.95CRHR1 antagonist 1
CAS :CRHR1 antagonist 1 (compound 10a) is a non-peptide antagonist of corticotropin-releasing hormone receptor 1 (CRHR1). It serves as a useful tool in the study of psychiatric disorders.Formule :C24H34N4OCouleur et forme :SolidMasse moléculaire :394.553Protease-Activated Receptor-1 antagonist 1
Compound 13 is a PAR-1 antagonist with a 3 nM IC50, useful for thrombosis and heart disease research.Formule :C25H24F2N2O3Couleur et forme :SolidMasse moléculaire :438.47VU0514009
CAS :VU0514009 is a competitive antagonist of chemokine-like receptor 1 (CMKLR1) with an EC50 of 2 nM. It effectively inhibits chemerin-9-induced arrestin recruitment and receptor internalization, significantly reducing Ca2+ flux responses in HEK293 cells. This compound shows potential for research in inflammatory diseases and metabolic syndrome.Formule :C21H20ClN3O5S2Couleur et forme :SolidMasse moléculaire :493.98Sitamaquine hydrochloride
CAS :Sitamaquine hydrochloride (WR 6026) is an orally active 8-aminoquinoline analog with antileishmanial activity. This compound inhibits mitochondrial complex II (succinate dehydrogenase) and is characterized by its lipophilic weak base properties. It rapidly accumulates in the acidic compartments of Leishmania parasites, predominantly localizing within the acidocalcisomes.Formule :C21H35Cl2N3OCouleur et forme :SolidMasse moléculaire :416.43Ophiobolin C
CAS :inhibitor of human CCR5 binding to HIV-1 gp120Formule :C25H38O3Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :386.57BI 703704
CAS :BI 703704, a soluble guanylate cyclase (sGC) activator, inhibits the progression of diabetic nephropathy in the ZSF1 rat [1].Formule :C32H37N3O4SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :559.72GnRH antagonist 2
CAS :GnRH antagonist 2 is a GnRH receptor antagonist, useful for studying endocrine diseases.Formule :C28H27F2N9O5Degré de pureté :98.08%Couleur et forme :SolidMasse moléculaire :607.57A3AR antagonist 5
CAS :A3AR antagonist 5 (Compound 16) acts as a selective antagonist for the human adenosine A3 receptor (human adenosine A3 receptor), with an affinity expressed as a pC value of 4.542 μM.Formule :C18H16N2O2SCouleur et forme :SolidMasse moléculaire :324.40Disulergine
CAS :Disulergine is a dopamine receptor agonist. It also prolactin release-inhibiting 8 alpha-amino-ergoline.Formule :C17H24N4O2SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :348.46Enprostil
CAS :Enprostil: synthetic PGE2 analog, reduces gastric acid, protects mucosa, lowers post-meal gastrin, treats ulcers effectively and safely.Formule :C23H28O6Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :400.46L 668750
CAS :L 668750 is an inhibitor of platelet-activating factor.Formule :C25H34O9SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :510.6S1P1 agonist 4
CAS :S1P1 agonist 4 exhibits enhanced potency with an EC 50 value of less than 0.05 mg/kg and a predicted human half-life (t1/2) of approximately 5 days, indicatingFormule :C24H31NO3Couleur et forme :SolidMasse moléculaire :381.51Atumelnant
CAS :Atumelnant (CRN04894) is an MC2R antagonist used in the study of congenital adrenocortical hyperplasia (CAH) and Cushing's disease (CD).Formule :C33H42F3N5O3Degré de pureté :98.41%Couleur et forme :SolidMasse moléculaire :613.71Henagliflozin
CAS :Henagliflozin (SHR3824): an oral, selective SGLT2 inhibitor, weak on SGLT1.Formule :C22H24ClFO7Couleur et forme :SolidMasse moléculaire :454.87Rodatristat ethyl
CAS :Rodatristat ethyl is an oral TPH1 inhibitor reducing 5-HT levels & lowering PAH at low doses.Formule :C29H31ClF3N5O3Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :590.04GHSR-1a agonist-1
CAS :GHSR-1a agonist-1 (Compound 4b) is an orally active agonist of the human growth hormone secretagogue receptor 1a (GHSR-1a) with an EC50 of 0.49 nM. It effectively stimulates the release of endogenous growth hormone by activating GHSR-1a. Doses as low as 0.1 mg/kg (administered orally) can increase body weight and length in 4-week-old rats. GHSR-1a agonist-1 is applicable in research on pediatric growth and developmental delays.Formule :C30H37N5O4Couleur et forme :SolidMasse moléculaire :531.6465-HT7R antagonist 3
CAS :Compound 6.4, also known as 5-HT7R antagonist 3, is a selective antagonist of the 5-HT7R with a Ki of 8 nM. It exhibits significantly less affinity towards D2R, 5-HT1AR, and 5-HT2AR with Ki values of 511 nM, 8930 nM, and 5786 nM, respectively. In mice, 5-HT7R antagonist 3 demonstrates anti-depressant and anti-anxiety activities.Formule :C30H33FN4O3Couleur et forme :SolidMasse moléculaire :516.61IMP-1575
CAS :IMP-1575 is a highly effective inhibitor of hedgehog acyltransferase (HHAT), with an IC50 of 0.75 μM when inhibiting purified HHAT. IMP-1575 has potential applications in cancer research.Formule :C19H25N3OSMasse moléculaire :343.49AAZ-A 154 hydrobromide
CAS :AAZ-A 154 hydrobromide is a selective, competitive, non-hallucinogenic 5-HT2AR antagonist. It promotes neuronal growth in rodents and yields enduring beneficial behavioral effects.Formule :C14H21BrN2OCouleur et forme :SolidMasse moléculaire :313.23AMG-369
CAS :AMG-369 (AMG 247) is an S1P1/S1P5 dual agonist that delays the development of experimental autoimmune encephalomyelitis in rats.Formule :C26H22FN3O2SDegré de pureté :98.04% - 98.92%Couleur et forme :SolidMasse moléculaire :459.54ChemR23-IN-3
ChemR23-IN-3 is a potent thiazole-based ChemR23 inhibitor with an IC 80 value of 12 nM.Formule :C31H33N5O5S2Couleur et forme :SolidMasse moléculaire :619.75PAR4 antagonist 3
CAS :PAR4 antagonist3 (Compound 36) is a selective antagonist of protease-activated receptor 4 (PAR4). It exhibits antiplatelet activity with an IC50 of 26.1 nM and enhances metabolic stability in human liver microsomes, with a half-life (T1/2) of 97.6 minutes.Formule :C22H16FN3O5SMasse moléculaire :453.44YM-49598 iodide
CAS :YM-49598 iodide is a tachykinin NK-1 receptor antagonist. It inhibits drug-induced bladder contractions in rats with an IC50 of 11 μg/kg.Formule :C36H45Cl2IN2O2Couleur et forme :SolidMasse moléculaire :735.57YM-31636 free base
CAS :YM-31636 (free base) is an orally active, potent, and selective agonist of the 5-HT3 receptor with a pKi value of 9.67. This compound induces contraction in isolated guinea pig distal colon and provokes tachycardia in isolated guinea pig right atrium, demonstrating a relative intrinsic activity of about 0.23. YM-31636 (free base) holds potential for research in constipation management.Formule :C14H11N3SCouleur et forme :SolidMasse moléculaire :253.32SCH-900822
CAS :SCH-900822 is a potent and selective glucagon receptor antagonist.Formule :C34H43Cl2N7O2Couleur et forme :SolidMasse moléculaire :652.66Revexepride
CAS :Revexepride, a 5-HT4 agonist, may boost CYP3A4, used for treating GERD.Formule :C21H32ClN3O4Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :425.95HU-308
CAS :HU-308, a synthetic cannabinoid analogue, is a highly selective agonist of the CB2 receptor. It demonstrates an affinity for the CB2 receptor that is over 440 times greater than its affinity for the CB1 receptor, which are predominantly found in immune cells. This compound plays a crucial role in modulating the immunosuppressive effects of the endocannabinoid system (ECS). Additionally, HU-308 possesses anti-inflammatory and neuroprotective properties, and it regulates the function of microglia. Its potential applications include research into neuroinflammation and retinal diseases.
Formule :C27H42O3Couleur et forme :SolidMasse moléculaire :414.62Histamine H3 antagonist-1
CAS :Compound 10o, a histamine H3 antagonist-1, functions as both a histamine H3 antagonist and a serotonin reuptake inhibitor, making it useful for research in depression [1].
Formule :C24H28F3N3O2Couleur et forme :SolidMasse moléculaire :447.49GLP-1 receptor agonist 12
CAS :Compound 20A, known as GLP-1 receptor agonist 12, acts as an agonist of the GLP receptor. It is utilized in researching diseases like diabetes [1].Formule :C31H31FN6O4Masse moléculaire :570.61TM38837
CAS :CB1 antagonist 4 is an inverse agonist of cannabinoid receptor 1 (CB1) with an IC50 of 0.4 nM. It can reduce body weight, improve plasma inflammatory markers, and enhance glucose homeostasis [1].
Formule :C27H20Cl2F3N7OCouleur et forme :SolidMasse moléculaire :586.40Neladenoson
CAS :Neladenoson is an effective and selective agonist of the Adenosine A1 Receptor (A1R). EGFR-IN-162 shows potential for research in heart failure.Formule :C29H24ClN5O2S2Couleur et forme :SolidMasse moléculaire :574.12ASN-1377642
CAS :ASN-1377642 is an NK1 receptor antagonist with a Ki value of 251 nM. It demonstrates antitumor activity in breast cancer cells with high expression of NK1R-Tr.Formule :C21H16ClN5OSCouleur et forme :SolidMasse moléculaire :421.905-HT2A receptor agonist-7
CAS :5-HT2A receptor agonist-7 (517) functions as a modulator of the 5-HT2A receptor, with an EC50 value of less than 100 nM.Formule :C12H11F2N3Couleur et forme :SolidMasse moléculaire :235.233RG-15
CAS :RG-15 is an orally active dopamine receptor antagonist with high affinity for the human D2 receptor (pKi of 8.23) and human D3 receptor (pKi of 10.49). It inhibits dopamine-stimulated [35S]GTPγS binding with IC50 values of 21.2 nM in rat striatal membranes, 36.7 nM in mouse A9 cells expressing human D2L receptors, and 7.2 nM in CHO cells expressing human D3 receptors. RG-15 enhances dopamine turnover and synthesis in the striatum and olfactory bulb of mice, exhibiting antipsychotic activity.Formule :C25H32Cl2F3N5O2SCouleur et forme :SolidMasse moléculaire :594.52HU 433
CAS :HU 433, a synthetic cannabinoid, acts as a CB2 receptor agonist and is an enantiomer of HU 308. It provides anti-inflammatory and neuroprotective effects by binding to the CB2 receptor, primarily found on immune cells, thereby modulating immune responses and inflammation. Additionally, HU 433 influences microglial signaling pathways, particularly LPS and IFNγ-mediated routes, affecting the phosphorylation of MAPKs, including ERK1/2, JNK, p38, and Akt. This compound is valuable in researching neuroinflammation and retinal diseases.Formule :C27H42O3Couleur et forme :SolidMasse moléculaire :414.62(2R,3S)-Azelaprag
CAS :(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide is an Apelin receptor agonistFormule :C25H29N7O4SDegré de pureté :97.47% - >99.99%Couleur et forme :SoildMasse moléculaire :523.61NBI 35965 hydrochloride
CAS :NBI 35965 hydrochloride is a selective CRF1 (corticotropin-releasing factor receptor 1) antagonist that is both orally active and capable of penetrating the brain. It possesses a K i value of 4 nM and a pK i of 8.5, and does not affect CRF2. This compound effectively diminishes CRF or stress-triggered ACTH (adrenocorticotropic hormone) production in vivo, demonstrating pIC 50 values of 7.1 and 6.9. Additionally, NBI 35965 hydrochloride exhibits anxiolytic properties [1] [2].Formule :C21H23Cl3N4Couleur et forme :SolidMasse moléculaire :437.79SSTR5 antagonist 6
CAS :SSTR5 antagonist 6, an orally active antagonist specific to the somatostatin receptor subtype 5 (SSTR5), exhibits an IC50 value of 24 nM. This compound is utilized in researching type 2 diabetes [1].Formule :C22H28ClN3O4Couleur et forme :SolidMasse moléculaire :433.93SJPYT-310
CAS :SJPYT-310 is a selective PXR antagonist, exhibiting no noticeable cytotoxicity.Formule :C27H36N4O3Couleur et forme :SolidMasse moléculaire :464.6Acyline
CAS :Acyline, a GnRH antagonist, suppresses gonadotropins and testosterone in animals and maintains the effect for 2 weeks in men with one dose.Formule :C80H102ClN15O14Couleur et forme :SolidMasse moléculaire :1533.211'-Naphthoyl-2-methylindole
CAS :1'-Naphthoyl-2-methylindole (Compound 88) acts as a cannabinoid mimic and an inhibitor of Win 55212-2, displaying a 34% inhibition of [3H]Win 55212-2 binding to cannabinoid receptors at a concentration of 3 μM.Formule :C20H15NOCouleur et forme :SolidMasse moléculaire :285.34GLP-1 receptor agonist 11
CAS :GLP-1 Receptor Agonist 11 (compound 3) acts as an effective agonist for the GLP Receptor, finding use in research related to conditions like diabetes and non-alc. fatty liver disease [1].Formule :C31H31ClFN3O4Couleur et forme :SolidMasse moléculaire :564.05Anti-MRSA agent 19
CAS :Anti-MRSA agent 19 (Compound 1) is an antibiotic that exhibits activity against Staphylococcus aureus. It is active against 40 clinical isolates from the CDC, representing diverse bacterial species with various resistance factors, including resistance to vancomycin, aminoglycoside/tetracycline, and oxazolidinone (median MIC=4 μg/mL).Formule :C15H10Cl3NO4Couleur et forme :SolidMasse moléculaire :374.6EP-3945
CAS :EP-3945 is an agonist of Mas-related G protein-coupled receptors (MRGPR), exhibiting greater potency than the small molecule agonist β-Alanine targeting MRGPRD. MRGPRs play a crucial role in inflammatory itch and pain perception. These receptors interact with Gq (MRGPRX2, MRGPRX4, and MRGPRX1 are coupled with Gq; MRGPRX2 and MRGPRD couple with Gi), with EP-3945 having an EC50 value of 211.6 nM for Gq.Formule :C24H26N4O3Couleur et forme :SolidMasse moléculaire :418.488FDU-PB-22
CAS :FDU-PB-22, a novel synthetic cannabinoid, undergoes rapid metabolism in human liver microsomes (HLM) with a half-life of 12.4 minutes.Formule :C26H18FNO2Couleur et forme :SolidMasse moléculaire :395.43RGH-122
CAS :RGH-122 (compound 43), characterized as an orally active, potent, and selective hV1a receptor antagonist, demonstrates significant affinity with a K i value of 0.3 nM and an IC 50 of 0.9 nM. It exhibits microsomal stability, indicated by a CL int value of 13/28/25 μL/min/mg [1].Formule :C24H25ClN4O3Couleur et forme :SolidMasse moléculaire :452.93Tebideutorexant
CAS :Tebideutorexant, an orexin-1 receptor antagonist, shows anti-panic effects in rodents and humans, providing a tool for stress response and psychiatric research.Formule :C23H16D2F4N4O2Degré de pureté :98.89%Couleur et forme :SolidMasse moléculaire :460.42Rimegepant sulfate hydrate
CAS :Rimegepant (BMS-927711/BHV-3000): oral CGRP blocker for migraines, effective without vasoconstriction, beats placebo, well-tolerated.Formule :C56H64F4N12O13SCouleur et forme :SolidMasse moléculaire :1221.2526Mrgx2 antagonist-3
CAS :Mrgx2 antagonist-3 (Compound B-40) is a highly selective antagonist of the MrgX2 receptor, with an IC50 range of 0.042-2.5 nM. It blocks downstream G protein signaling and β-arrestin recruitment, inhibiting Mrgx2 receptor-mediated calcium influx and cell degranulation. Mrgx2 antagonist-3 shows potential for research in inflammation-associated diseases and pruritus, such as chronic urticaria and allergic asthma.Formule :C15H15F2N3OCouleur et forme :SolidMasse moléculaire :291.30GRK6-IN-5
CAS :GRK6-IN-5 is an inhibitor of the GRK6 polypeptide, with an IC50 of 4.48 μM. GRK6-IN-5 is utilized in research focused on hematological malignancies, inflammatory diseases, and autoimmune disorders.Formule :C23H21N3O2Couleur et forme :SolidMasse moléculaire :371.432MRGPRX2 modulator-1
CAS :MRGPRX2 modulator-1 (example 17), a modulator of the mas-related G-protein receptor X2 (MRGPRX2), is employed in studies focused on inflammation, pain, and autoimmune disorders [1].Formule :C20H19F6N5OCouleur et forme :SolidMasse moléculaire :459.39BIBO3304 diTFA
CAS :BIBO3304 (diTFA), a selective neuropeptide Y (NPY) Y1 receptor antagonist, demonstrates oral efficacy. It exhibits high affinity for Y1 receptors in both humans and rats, with IC50 values of 0.38 nM and 0.72 nM, respectively. Additionally, BIBO3304 (diTFA) enhances bone-tendon healing via the Wnt/β-catenin signaling pathway [1] [2] [3].Formule :C33H37F6N7O7Couleur et forme :SolidMasse moléculaire :757.68H-Glu-Thr-OH
CAS :H-Glu-Thr-OH (L-α-Glutamyl-L-threonine) is a dipeptide composed of two amino acids—glutamic acid (Glu) and threonine (Thr)—linked by a peptide bond and functions as an agonist of the extracellular calcium-sensing receptor (CaSR).Formule :C9H16N2O6Couleur et forme :SolidMasse moléculaire :248.23Tiprenolol hydrochloride
CAS :Tiprenolol hydrochloride is a β-adrenoceptor (β-adrenoceptor) antagonist. This compound is effective in eliminating ventricular arrhythmias in dogs caused by intravenous administration of adrenaline, following inhalation of halothane.Formule :C13H22ClNO2SCouleur et forme :SolidMasse moléculaire :291.84CI-988
CAS :CCK2 (CCK-B) receptor antagonistFormule :C35H42N4O6Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :614.73SSR-241586
CAS :SSR-241586: Neurokinin antagonist, treats depression, schizophrenia, urinary issues, emesis, IBS.Formule :C32H42Cl2N4O3Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :601.61Mesulergine hydrochloride
CAS :5-HT2A and 2C receptor antagonistFormule :C18H27ClN4O2SDegré de pureté :98%Couleur et forme :SolidMasse moléculaire :398.95ADORA2A/PDE4D-IN-1
CAS :ADORA2A/PDE4D-IN-1 (Compound 9) is a dual inhibitor of the adenosine A2a receptor (ADORA2A) and phosphodiesterase 4D (PDE4D). This compound is applicable for research in bronchial asthma.Formule :C14H11N5Couleur et forme :SolidMasse moléculaire :249.271S1P1 agonist 5
Selective oral S1P1 agonist 5 inhibits lymphocyte drainage, potential for MS research.Formule :C23H24ClN2NaO4Couleur et forme :SolidMasse moléculaire :450.895-HT1A antagonist 1
Compound 6f is a potent, selective 5-HT1A receptor blocker (Ki: 35 nM), useful in CNS disorder research.Formule :C23H29ClN6O2Couleur et forme :SolidMasse moléculaire :456.97ATL444
CAS :ATL444 is an adenosine receptor antagonist with affinity (Ki values) for rA1AR, rA2AAR, rA2BAR, and rA3AR of 7.0, 2.5, 61.8, and >1000 nM, respectively.Formule :C17H19N5OCouleur et forme :SolidMasse moléculaire :309.37R-137696
CAS :R-137696 is an orally active 5-HT1A receptor agonist that facilitates the relaxation of the proximal stomach. It is utilized in research related to functional dyspepsia.Formule :C17H23N3O2Couleur et forme :SolidMasse moléculaire :301.38Flucopride
CAS :Flucopride (Compound 4a) acts as an acetylcholinesterase inhibitor (AChE) with an IC50 value of 24 nM and serves as a partial agonist for the human 5-HT4 receptor (5-HT4R) with a Ki of 9.6 nM for (h)5-HT4R. It promotes non-amyloidogenic processing of APP in COS-7 cells transiently expressing (h)5-HT4R with an EC50 of 23.0 nM. Flucopride is also likely to exhibit significant gastrointestinal tract (GIT) penetration and blood-brain barrier (BBB) permeability, as determined in PAMPA experiments.Formule :C22H33FN2O2Couleur et forme :SolidMasse moléculaire :376.51Iralukast (CGP 45715A)
CAS :Iralukast is a cysteinyl-leukotriene antagonist (CysLT) with a pKi of 7.8 for CysLT1.Formule :C38H37F3O8SCouleur et forme :SolidMasse moléculaire :710.76A2A receptor antagonist 2
A2A receptor antagonist 2 is a highly selective and potent antagonist of the adenosine A2Areceptor (IC50: 8.3 nM).Formule :C25H28FN7O3Couleur et forme :SolidMasse moléculaire :493.53AGH-107
CAS :AGH-107 is a highly selective 5-HT7 receptor agonist that can cross the blood-brain barrier, featuring a Ki value of 6 nM and an EC50 value of 19 nM. Demonstrating high selectivity for central nervous system targets, AGH-107 also exhibits high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.Formule :C13H12IN3Couleur et forme :SolidMasse moléculaire :337.16Tipindole
CAS :Tipindole is a serotonin antagonist utilized in research related to depression.Formule :C16H20N2O2SCouleur et forme :SolidMasse moléculaire :304.41Sulfinalol hydrochloride
CAS :Sulfinalol hydrochloride is an orally active β-adrenoceptor (β-adrenoceptor) antagonist that exhibits direct vasodilatory activity. It is also classified as an antihypertensive agent.Formule :C20H28ClNO4SCouleur et forme :SolidMasse moléculaire :413.96CCR1 antagonist 11 hydrochloride
Oral CCR1 antagonist A1B1 targets h/m/rCCR1 (IC50: 0.03/0.58/0.32 μM), potential for treating inflammatory diseases.Couleur et forme :SolidA1AR antagonist 1
Compound 18g, a potent A1AR blocker with Ki: 2.08 nM (hA1), 6.91 nM (hA2A), 31.2 nM (hA2B).Formule :C18H14N4OCouleur et forme :SolidMasse moléculaire :302.33Bometolol Hydrochloride
CAS :Bometolol Hydrochloride is a beta-adrenergic blocking compound used for the treatment of cardiovascular disease.Formule :C25H33ClN2O7Degré de pureté :98%Couleur et forme :SolidMasse moléculaire :508.99THRX-194556
CAS :THRX-194556 is an agonist of the 5-HT4 receptor. It is applicable in the study of gastrointestinal functional disorders and Alzheimer's disease.Formule :C28H41N5O5SCouleur et forme :SolidMasse moléculaire :559.721RGS10 modulator-1
CAS :RGS10 modulator-1 (compound 15) is an effective regulator of RGS10. It significantly reverses IFNγ-induced expression of both RGS10 protein and mRNA, as well as COX-2 mRNA and iNOS expression triggered by IFNγ.Formule :C16H15BrN2O3S2Couleur et forme :SolidMasse moléculaire :427.336AAZ-A 154 hydrochloride
CAS :AAZ-A 154 hydrochloride is a selective, competitive, non-hallucinogenic antagonist of 5-HT2AR. It promotes neuronal growth in rodents and results in enduring beneficial behavioral effects.Formule :C14H21ClN2OCouleur et forme :SolidMasse moléculaire :268.78SSTR4 agonist 5
CAS :SSTR4 agonist5 (Compound 5) is an orally active agonist of the somatostatin receptor 4 (SSTR4) with an EC50 of 0.228 nM. It demonstrates good stability in human/rat liver microsomes and can inhibit mechanical hyperalgesia in rat models.Formule :C20H26N4OMasse moléculaire :338.447
