GPCR/Proteína-G
Os inibidores de GPCR/proteínas G são compostos que têm como alvo os receptores acoplados a proteínas G (GPCRs) e as proteínas G associadas, que desempenham papéis críticos na transmissão de sinais do exterior para o interior das células. Esses inibidores são essenciais para estudar as vias de sinalização mediadas por GPCRs, que estão envolvidas em numerosos processos fisiológicos, incluindo percepção sensorial, resposta imunológica e neurotransmissão. Os inibidores de GPCR também são importantes no desenvolvimento de medicamentos, pois muitos agentes terapêuticos têm como alvo esses receptores. Na CymitQuimica, oferecemos uma ampla gama de inibidores de GPCR/proteínas G de alta qualidade para apoiar sua pesquisa em farmacologia, biologia celular e áreas afins.
Subcategorias de "GPCR/Proteína-G"
- Receptor 5-HT(939 produtos)
- Receptor de adenosina(242 produtos)
- Receptor adrenérgico(2.943 produtos)
- Receptor de Bombesina(30 produtos)
- Receptor de Bradicinina(59 produtos)
- CXCR(148 produtos)
- CaSR(32 produtos)
- Receptor de Canabinóides(196 produtos)
- Receptor de Dopamina(407 produtos)
- Receptor Endotelina(76 produtos)
- Receptor GNRH(69 produtos)
- GPCR19(31 produtos)
- GRK(31 produtos)
- GTPase(21 produtos)
- Receptor Glucagon(164 produtos)
- Hedgehog/Smoothened(44 produtos)
- Receptor de Histamina(358 produtos)
- Receptor LPA(21 produtos)
- Receptor de Melatonina(24 produtos)
- Receptor OX(40 produtos)
- Receptor opioide(297 produtos)
- PAFR(11 produtos)
- PKA(48 produtos)
- Receptor S1P(17 produtos)
- SGLT(30 produtos)
- Receptor Sigma(46 produtos)
Exibir 18 mais subcategorias
Foram encontrados 5337 produtos de "GPCR/Proteína-G"
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PD 136450
CAS:<p>PD-136,450: partial stomach secretory agonist, full pancreas agonist in rats; potential acid-reducing drug, adjuvant for gastrin-sensitive tumors.</p>Fórmula:C35H40N4O6Pureza:98%Cor e Forma:SolidPeso molecular:612.72NK1 receptor antagonist 2
CAS:<p>NK1 Receptor Antagonist 2, a compound targeting the NK1 receptor, holds potential for tinnitus and hearing loss research.</p>Fórmula:C31H35F7N4O2Cor e Forma:SolidPeso molecular:628.62BI-685509
CAS:<p>BI-685509: potent, oral sGC activator, boosts cGMP, enhances NO pathways, for CKD/DKD research.</p>Fórmula:C34H38N4O5Cor e Forma:SolidPeso molecular:582.69EP4 receptor antagonist 7
CAS:<p>EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4, with an IC50 of 1.1 nM. This compound inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 of 0.9 nM. In RAW 264.7 macrophages, it reduces the expression of PGE2-induced IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C motif) ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase 1 (Arg1) mRNA. In the CT26 mouse colon cancer model, EP4 receptor antagonist 7, combined with an anti-PD-1 antibody, inhibits tumor growth and enhances CD8+ T cell infiltration into the tumor.</p>Fórmula:C24H18F3N3O3Cor e Forma:SolidPeso molecular:453.413D3/5-HT receptor modulator-1
CAS:<p>D3/5-HT receptor modulator-1 (compound 5i) is a selective antagonist of the dopamine D3 and 5-HT2A receptors, and a partial agonist at the 5-HT1A receptor. It exhibits Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for the dopamine D3, 5-HT2A, and 5-HT1A receptors respectively. The compound shows lower affinity for the dopamine D2 receptor, 5-HT2C receptor, and hERG channel. D3/5-HT receptor modulator-1 possesses atypical antipsychotic properties.</p>Fórmula:C24H29N3O2Cor e Forma:SolidPeso molecular:391.506TM38837
CAS:<p>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].</p>Fórmula:C27H20Cl2F3N7OCor e Forma:SolidPeso molecular:586.40CCR1 antagonist 13
CAS:<p>CCR1 antagonist13 is a selective small molecule antagonist of CCR1.</p>Fórmula:C25H27ClFN3O4Cor e Forma:SolidPeso molecular:487.95ASN-1377642
CAS:<p>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.</p>Fórmula:C21H16ClN5OSCor e Forma:SolidPeso molecular:421.90L-796778 acetate
CAS:<p>L-796778 acetate is a selective sst3 receptor agonist. In CHO-K1 cells expressing hsst3 receptors, it acts as a partial agonist that inhibits Forskolin-induced cAMP production, with an IC50 value of 18 nM. Additionally, L-796778 acetate exhibits anticonvulsant properties.</p>Fórmula:C31H44N6O9Cor e Forma:SolidPeso molecular:644.716Aplaviroc hydrochloride
CAS:<p>Aplaviroc, a potent CCR5 inhibitor, binds selectively, blocking HIV entry and specific monoclonal antibody attachment in vitro.</p>Fórmula:C33H44ClN3O6Cor e Forma:SolidPeso molecular:614.17INCB-9471 dihydrochloride
CAS:<p>INCB-9471 HCl: a potent CCR5 antagonist, blocks monocyte migration & HIV-1.</p>Fórmula:C30H42Cl2F3N5O2Pureza:98%Cor e Forma:SolidPeso molecular:632.59Kendomycin
CAS:<p>Kendomycin is a proteasome inhibitor and endothelin receptor antagonist. It induces apoptosis in lymphoma.</p>Fórmula:C29H42O6Cor e Forma:SolidPeso molecular:486.64Dopamine D3 receptor antagonist-1
<p>Dopamine D3 receptor antagonist-1 is a dopamine D3 receptor selective or multi-targeting ligand with a Ki value of 1.58 nM that has demonstrated therapeutic</p>Fórmula:C31H35Cl2N3O3Cor e Forma:SolidPeso molecular:568.53(R)-BAY-899
<p>(R)-BAY-899: R-isomer, selective LH-R antagonist, effective on hLH (IC50: 185 nM) and rLH (IC50: 46 nM), orally active.</p>Fórmula:C25H19F2N5O2Cor e Forma:SolidPeso molecular:459.45BRL-37344
CAS:<p>BRL-37344 is a selective β3-adrenergic receptor agonist. It significantly reduces the body weight of obese mice.</p>Fórmula:C19H22ClNO4Cor e Forma:SolidPeso molecular:363.84Y1 receptor antagonist 1
CAS:<p>Y1 receptor antagonist 1 is an antagonist of neuropeptide Y1 receptor.</p>Fórmula:C28H33N5O3Pureza:98.17%Cor e Forma:SolidPeso molecular:487.59DMPX
CAS:<p>DMPX (3,7-Dimethyl-1-propargylxanthine) is a caffeine-like compound capable of crossing the blood-brain barrier. It serves as an A2-selective adenosine receptor (AR) antagonist, effectively and selectively blocking the hypothermia and behavioral inhibition induced by A2 adenosine receptor agonists, such as NECA. DMPX is utilized in research on diseases like Parkinson's disease.</p>Fórmula:C10H10N4O2Cor e Forma:SolidPeso molecular:218.212BAY 38-7271
CAS:<p>BAY 38-7271: potent neuroprotective, selective CB1/CB2 agonist, Ki of 1.85 nM (CB1) & 5.96 nM (CB2).</p>Fórmula:C20H21F3O5SPureza:98%Cor e Forma:SolidPeso molecular:430.44AAZ-A 154 hydrochloride
CAS:<p>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.</p>Fórmula:C14H21ClN2OCor e Forma:SolidPeso molecular:268.78AAZ-A 154 hydrobromide
CAS:<p>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.</p>Fórmula:C14H21BrN2OCor e Forma:SolidPeso molecular:313.23A3AR antagonist 5
CAS:<p>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.</p>Fórmula:C18H16N2O2SCor e Forma:SolidPeso molecular:324.40Nedocromil sodium
CAS:<p>Nedocromil sodium is a pharmacologic stabilizer of mast cells, has been shown to normalize cytokine levels and attenuate cardiac remodeling.</p>Fórmula:C19H17NNaO7Pureza:98%Cor e Forma:SolidPeso molecular:394.335P2Y14R antagonist 4
CAS:<p>Compound 25l, also known as P2Y14R antagonist 4, is an orally active antagonist of the P2Y14R receptor with an IC50 of 5.6 nM. It exhibits higher binding affinity for P2Y14R compared to other PPTN receptors. P2Y14R antagonist 4 also possesses anti-inflammatory properties, reducing the release of pro-inflammatory cytokines (IL-1β, IL-6, and TNF-α) induced by LPS.</p>Fórmula:C27H27F3N2O4SCor e Forma:SolidPeso molecular:532.574S1PR1 agonist 2
CAS:<p>S1PR1 agonist 2 is potent for autoimmune research (from WO2021175225A1).</p>Fórmula:C25H25N5O4Cor e Forma:SolidPeso molecular:459.50Toladryl
CAS:<p>Toladryl is a derivative of Diphenhydramine that can cross the blood-brain barrier and exhibits oral activity, with antihistamine and anticholinergic properties. Its anticholinergic effects are approximately a tenth of those seen with Diphenhydramine, yet it offers 2-4 times the protection against lethal doses of histamine in guinea pigs. The side effects of Toladryl are fewer and milder compared to Diphenhydramine; however, at higher doses, it may cause symptoms such as insomnia, agitation, and disorientation related to the central nervous system. Toladryl is utilized in the research of allergic diseases.</p>Fórmula:C18H23NOCor e Forma:SolidPeso molecular:269.38BNS808
CAS:<p>BNS808 is an orally active, selective CB1R antagonist with an IC50 of 0.8 nM, demonstrating significant selectivity for CB2R and minimal brain penetration. It is being studied for the treatment of obesity and related metabolic complications, such as metabolic dysfunction-associated steatotic liver disease (MASLD). BNS808 reduces drug exposure to the central nervous system, enhancing safety, and minimizes drug interactions through high plasma protein binding.</p>Fórmula:C25H20Cl3N3O3SCor e Forma:SolidPeso molecular:548.869SSTR5 antagonist 2 TFA
CAS:<p>Potent, oral SSTR5 antagonist 2 TFA may treat type 2 diabetes.</p>Fórmula:C34H36F4N2O7Pureza:98%Cor e Forma:SolidPeso molecular:660.65PAR-2-IN-2
CAS:<p>PAR-2-IN-2 (compound P-596) is an inhibitor of protease-activated receptor 2 (PAR-2), with an IC50 of 10.79 μM for SLIGKV and an IC50 greater than 200 μM for trypsin.</p>Fórmula:C25H20F3N5O2Cor e Forma:SolidPeso molecular:479.454Teoprolol
CAS:<p>Teoprolol is a blocker of β-adrenergic receptor.</p>Fórmula:C23H30N6O4Pureza:98%Cor e Forma:SolidPeso molecular:454.52Rodatristat ethyl
CAS:<p>Rodatristat ethyl is an oral TPH1 inhibitor reducing 5-HT levels & lowering PAH at low doses.</p>Fórmula:C29H31ClF3N5O3Pureza:98%Cor e Forma:SolidPeso molecular:590.04TAK-075
CAS:<p>TAK-075 is an orally active CaSR antagonist with an IC50 value of 0.94 nM. It transiently stimulates parathyroid hormone (PTH) secretion in rats and effectively prevents significant reduction in PTH secretion due to the accumulation of active metabolites, thereby maintaining a normal secretion pattern. TAK-075 is applicable in research related to metabolic diseases and osteoporosis.</p>Fórmula:C36H46N4O4SCor e Forma:SolidPeso molecular:630.84NBI 35965 hydrochloride
CAS:<p>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].</p>Fórmula:C21H23Cl3N4Cor e Forma:SolidPeso molecular:437.79YM158 free base
CAS:<p>YM158 free base is a potent and selective antagonist of TXA2 and LTD4 receptor (pA2s: about 8.81 and 8.87).</p>Fórmula:C32H33ClN6O5S2Pureza:98%Cor e Forma:SolidPeso molecular:681.22DSP-1053 benzenesulfonate
CAS:<p>DSP-1053: Benzylpiperidine-based, potent SERT inhibitor (Ki=1.02nM), partial 5-HT1A receptor agonist (Ki=5.05nM), antidepressant.</p>Fórmula:C32H38BrNO7SCor e Forma:SolidPeso molecular:660.62SSTR5 antagonist 6
CAS:<p>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].</p>Fórmula:C22H28ClN3O4Cor e Forma:SolidPeso molecular:433.93U91356
CAS:<p>U91356 is an agonist of the dopamine receptors.</p>Fórmula:C13H17N3OPureza:98%Cor e Forma:SolidPeso molecular:231.29MK-0812
CAS:<p>MK-0812 is a dual antagonist of the CCR2 and CCR5 receptors that can alleviate adipose inflammation in ob/ob mice.</p>Fórmula:C24H34F3N3O3Pureza:98%Cor e Forma:SolidPeso molecular:469.54GAT564
<p>GAT564, an allosteric CB1R modulator, shows EC50s of 87 nM (cAMP) & 320 nM (β-arrestin2) and lowers IOP effectively in glaucoma mice.</p>Fórmula:C20H16N2O2SCor e Forma:SolidPeso molecular:348.4225B-NBOH hydrochloride
CAS:<p>25B-NBOH hydrochloride is a phenethylamine that exhibits high affinity for serotonin (5-HT) receptors 5-HT2A and 5-HT2C, with pKi values of 8.3 and 9.4, respectively.</p>Fórmula:C17H21BrClNO3Cor e Forma:SolidPeso molecular:402.711MRGPRX1 agonist 3
<p>Compound 1f, a potent MRGPRX1 agonist, has an EC50 of 0.22 μM, useful for neuropathic pain studies.</p>Fórmula:C14H11FN2OSCor e Forma:SolidPeso molecular:274.31GRK6-IN-4
CAS:<p>GRK6-IN-4 is an inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 value of 1.56 μM. GRK6-IN-4 is applicable for research related to hematological malignancies, inflammatory diseases, and autoimmune disorders.</p>Fórmula:C15H15N5Cor e Forma:SolidPeso molecular:265.313SB 224289
CAS:<p>SB 224289: selective 5-HT1B antagonist, pKi 8.2, 60x selectivity, effective orally.</p>Fórmula:C32H32N4O3Pureza:98%Cor e Forma:SolidPeso molecular:520.62Ici D1542
CAS:<p>Ici D1542: potent TXS inhibitor & TXA2 receptor antagonist, effective thromboxane blocker in vitro.</p>Fórmula:C25H30N2O7Pureza:98%Cor e Forma:SolidPeso molecular:470.51Protease-Activated Receptor-1 antagonist 2
<p>Selective, orally active PAR-1 antagonist with an IC50 of 7 nM, potential for cardiovascular disease studies.</p>Cor e Forma:SolidSSTR4 agonist 4
CAS:<p>SSTR4 agonist 4, potent in pain research, shows promise in rodent pain models, with potential for Alzheimer's due to hippocampus activity.</p>Fórmula:C19H26N4OCor e Forma:SolidPeso molecular:326.44UK-432097
CAS:<p>UK 432097 is an adenosine A2A agonist.</p>Fórmula:C40H47N11O6Cor e Forma:SolidPeso molecular:777.87TAK-024
CAS:TAK-024 is an inhibitor of platelet(IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively).Fórmula:C27H34N10O6Pureza:98%Cor e Forma:SolidPeso molecular:594.62MK-8318
CAS:<p>MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).</p>Fórmula:C27H26F4N2O5Pureza:98%Cor e Forma:SolidPeso molecular:534.5APJ receptor agonist 3
CAS:<p>APJ receptor agonist 3 is a highly effective and orally administerable agonist of the APJ receptor, demonstrating a potent EC50 value of 0.027 nM.</p>Fórmula:C26H29ClN4O5Cor e Forma:SolidPeso molecular:512.98(-)-5-HT2C agonist-3
CAS:<p>Compound (−)-19, also known as (-)-5-HT2C agonist-3, is a selective 5-HT2C agonist exhibiting a preference for Gq signaling. It demonstrates efficiency with EC50 values for 5-HT2 receptor subtypes as follows: 5-HT2C at 103 nM, 5-HT2B at 570 nM, and 5-HT2A at 72 nM. This compound is utilized in research on antipsychotics.</p>Fórmula:C19H23ClFNO2Cor e Forma:SolidPeso molecular:351.84
