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Proteina G/GPCR

Proteina G/GPCR

Gli inibitori dei GPCR/proteine G sono composti che bersagliano i recettori accoppiati alle proteine G (GPCR) e le proteine G associate, che svolgono ruoli critici nella trasmissione dei segnali dall'esterno all'interno delle cellule. Questi inibitori sono essenziali per studiare le vie di segnalazione mediate dai GPCR, coinvolte in numerosi processi fisiologici, tra cui la percezione sensoriale, la risposta immunitaria e la neurotrasmissione. Gli inibitori dei GPCR sono anche importanti nello sviluppo di farmaci, poiché molti agenti terapeutici prendono di mira questi recettori. Presso CymitQuimica, offriamo una vasta gamma di inibitori dei GPCR/proteine G di alta qualità per supportare le tue ricerche in farmacologia, biologia cellulare e campi correlati.

Sottocategorie di "Proteina G/GPCR"

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Trovati 5745 prodotti di "Proteina G/GPCR"

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  • ADORA2A/PDE4D-IN-1

    CAS:
    <p>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.</p>
    Formula:C14H11N5
    Colore e forma:Solid
    Peso molecolare:249.271
  • Mesulergine hydrochloride

    CAS:
    5-HT2A and 2C receptor antagonist
    Formula:C18H27ClN4O2S
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:398.95
  • SSR-241586

    CAS:
    SSR-241586: Neurokinin antagonist, treats depression, schizophrenia, urinary issues, emesis, IBS.
    Formula:C32H42Cl2N4O3
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:601.61
  • CI-988

    CAS:
    CCK2 (CCK-B) receptor antagonist
    Formula:C35H42N4O6
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:614.73
  • Leukotriene F4

    CAS:
    LTF4, made in vitro from LTE4 with enzymes, contracts vascular muscle weakly; potency is LTD4 > LTC4 > LTE4 >> LTF4.
    Formula:C28H44N2O8S
    Colore e forma:Solid
    Peso molecolare:568.72
  • Revexepride

    CAS:
    Revexepride, a 5-HT4 agonist, may boost CYP3A4, used for treating GERD.
    Formula:C21H32ClN3O4
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:425.95
  • SCH-900822

    CAS:
    SCH-900822 is a potent and selective glucagon receptor antagonist.
    Formula:C34H43Cl2N7O2
    Colore e forma:Solid
    Peso molecolare:652.66
  • GHSR-1a agonist-1

    CAS:
    <p>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.</p>
    Formula:C30H37N5O4
    Colore e forma:Solid
    Peso molecolare:531.646
  • Henagliflozin

    CAS:
    Henagliflozin (SHR3824): an oral, selective SGLT2 inhibitor, weak on SGLT1.
    Formula:C22H24ClFO7
    Colore e forma:Solid
    Peso molecolare:454.87
  • BI 703704

    CAS:
    <p>BI 703704, a soluble guanylate cyclase (sGC) activator, inhibits the progression of diabetic nephropathy in the ZSF1 rat [1].</p>
    Formula:C32H37N3O4S
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:559.72
  • PF-00446687

    CAS:
    PF-00446687 is a selective agonist of melanocortin-4 receptor (MC4R) (EC50 of 12 ± 1 nM).
    Formula:C28H36F2N2O2
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:470.59
  • Aplaviroc

    CAS:
    Aplaviroc (AK 602), a SDP derivative, is a CCR5 antagonist. With IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW.
    Formula:C33H43N3O6
    Purezza:97.98% - 98.26%
    Colore e forma:Solid
    Peso molecolare:577.71
  • GLP-1R agonist 8

    CAS:
    <p>GLP-1R agonist 8 is a potent agonist of GLP-1R (EC50 &lt; 2 nM).</p>
    Formula:C33H32N4O5
    Colore e forma:Solid
    Peso molecolare:564.63
  • Butaprost

    CAS:
    Butaprost: EP2 receptor agonist, EC50=33 nM, Ki=2.4 μM (murine), reduces fibrosis via TGF-β/Smad2.
    Formula:C24H40O5
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:408.57
  • P2Y14R 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>
    Formula:C27H27F3N2O4S
    Colore e forma:Solid
    Peso molecolare:532.574
  • LY 292728

    CAS:
    LY 292728 is a highly potent antagonist of leukotriene B4 receptor.
    Formula:C34H29FO9
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:600.59
  • LPA2 antagonist 5

    CAS:
    LPA2 antagonist 5 (EX1) functions as an antagonist of LPA2, with an IC50 value of 4.05 nM.
    Formula:C17H17F3N2O5
    Colore e forma:Solid
    Peso molecolare:386.323
  • DMPX

    CAS:
    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.
    Formula:C10H10N4O2
    Colore e forma:Solid
    Peso molecolare:218.212
  • BMS-986104 HCl

    CAS:
    BMS-986104 is a potent and selective S1P1 receptor modulator.
    Formula:C22H36ClNO
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:365.98
  • MRS7799

    CAS:
    <p>MRS7799 is a selective A3 Adenosine Receptor antagonist with Kd values of 0.55 nM for humans, 3.74 nM for mice, and 2.80 nM for rats. MRS7799 can be utilized in research related to neurodegenerative diseases, cancer, cardiac and cerebral ischemia, and autoimmune inflammatory diseases.</p>
    Formula:C22H18N4OS
    Colore e forma:Solid
    Peso molecolare:386.47
  • 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>
    Formula:C35H40N4O6
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:612.72
  • Nedocromil sodium

    CAS:
    Nedocromil sodium is a pharmacologic stabilizer of mast cells, has been shown to normalize cytokine levels and attenuate cardiac remodeling.
    Formula:C19H17NNaO7
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:394.335
  • IRL 2500

    CAS:
    <p>IRL 2500 is an antagonist of Endothelin receptor with IC50s of 1.3 and 94 nM for Endothelin A receptor and Endothelin B receptor.</p>
    Formula:C36H35N3O4
    Purezza:99.36%
    Colore e forma:White Crystalline Solid
    Peso molecolare:573.68
  • TAK-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>
    Formula:C36H46N4O4S
    Colore e forma:Solid
    Peso molecolare:630.84
  • (1R,2S,3R)-Aprepitant

    CAS:
    <p>(1R,2S,3R)-Aprepitant (Compound ent-4) is a competitive antagonist of the human neurokinin-1 (NK-1) receptor. It holds potential for research in the treatment of nausea and vomiting related to cancer or postoperative conditions.</p>
    Formula:C23H21F7N4O3
    Colore e forma:Solid
    Peso molecolare:534.427
  • Ici D1542

    CAS:
    Ici D1542: potent TXS inhibitor & TXA2 receptor antagonist, effective thromboxane blocker in vitro.
    Formula:C25H30N2O7
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:470.51
  • Abarelix acetate

    CAS:
    Abarelix acetate: synthetic GnRHR antagonist, spikes histamine, lowers LH and testosterone temporarily, used in advanced prostate cancer.
    Formula:C72H95ClN14O14·xC2H4O2
    Colore e forma:Solid
    Peso molecolare:1476.14
  • SR 140333

    CAS:
    SR 140333 is a NK1 receptor antagonist.
    Formula:C37H45Cl3N2O2
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:656.12
  • LP 12 hydrochloride hydrate


    LP 12 hydrochloride hydrate: potent, selective 5-HT7 agonist (Ki: 0.13 nM); less affinity for D2, 5-HT1A/2A receptors.
    Formula:C32H39N3O·HCl·xH2O
    Colore e forma:Solid
  • BNS808

    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>
    Formula:C25H20Cl3N3O3S
    Colore e forma:Solid
    Peso molecolare:548.869
  • CCR7 Ligand 1

    CAS:
    CCR7-Cmp2105 is a thiadiazole-dioxide allosteric antagonist for CCR7 with a Kd of 3 nM and IC50 of 7.3 μM against arrestin binding.
    Formula:C22H29N5O5S
    Colore e forma:Solid
    Peso molecolare:475.56
  • Pexacerfont

    CAS:
    Pexacerfont (BMS-562086) is a selective antagonist of the corticotropin-releasing factor receptor (IC50: 6.1±0.6 nM for the human CRF1 receptor).
    Formula:C18H24N6O
    Purezza:99.77%
    Colore e forma:Solid
    Peso molecolare:340.42
  • CB1/2 receptor-1

    CAS:
    CB1/2 receptor-1 (compound 5.3) serves as an agonist for CB1/2 receptors and is utilized in angiogenesis research.
    Formula:C33H48O2
    Colore e forma:Solid
    Peso molecolare:476.73
  • Bzo-poxizid

    CAS:
    Bzo-poxizid is a synthetic cannabinoid and a psychoactive substance.
    Formula:C20H21N3O2
    Colore e forma:Solid
    Peso molecolare:335.40
  • MED 27

    CAS:
    <p>MED 27 is an inhibitor of thromboxane synthase and thromboxane A2 receptors. It effectively inhibits rat platelet aggregation at doses significantly lower than those required for acetylsalicylic acid.</p>
    Formula:C24H25N5O5
    Colore e forma:Solid
    Peso molecolare:463.49
  • AAZ-A 154 mesylate

    CAS:
    <p>AAZ-A 154 mesylate mesylate is a selective, competitive, and non-hallucinogenic antagonist of 5-HT2AR. It enhances neuronal growth in rodents and produces enduring beneficial behavioral effects.</p>
    Formula:C15H24N2O4S
    Colore e forma:Solid
    Peso molecolare:328.43
  • LB-102

    CAS:
    LB-102 is an orally active inhibitor of dopamine D2, D3, and serotonin 5-HT7 receptors, utilized in the study of schizophrenia and other psychiatric disorders.
    Formula:C18H29N3O4S
    Colore e forma:Solid
    Peso molecolare:383.51
  • AAZ-A 154

    CAS:
    <p>AAZ-A 154 is a selective, competitive, and non-hallucinogenic antagonist of the 5-HT2AR. It promotes neuronal growth in rodents and results in lasting beneficial behavioral effects.</p>
    Formula:C14H20N2O
    Colore e forma:Solid
    Peso molecolare:232.32
  • Sigma-2 Radioligand 2

    CAS:
    Sigma-2 Radioligand 2 (compound 4) exhibits low nanomolar affinity for the σ2 receptor (Ki=2.30 nM) and high subtype selectivity (Ki(σ1)/Ki(σ2) > 1500).
    Formula:C23H28FN3O3
    Colore e forma:Solid
    Peso molecolare:413.49
  • AAZ-A 154 benzoate

    CAS:
    <p>AAZ-A 154 benzoate is a selective, competitive, and non-hallucinogenic 5-HT2AR antagonist. This compound facilitates neuronal growth in rodents and produces lasting beneficial behavioral effects.</p>
    Formula:C21H26N2O3
    Colore e forma:Solid
    Peso molecolare:354.44
  • Protease-Activated Receptor-1 antagonist 3


    PAR-1 antagonist 3: potent (IC50: 7 nM), binds hERG K+ channels (IC50: 9 μM).
    Formula:C30H34N4O3
    Colore e forma:Solid
    Peso molecolare:498.62
  • BMS-741672

    CAS:
    <p>BMS-741672 is a potent, selective CCR2 antagonist for the treatment of neuropathic pain.</p>
    Formula:C25H33F3N6O2
    Colore e forma:Solid
    Peso molecolare:506.56
  • NCATS-SM4420

    CAS:
    <p>NCATS-SM4420 (Compound A35) is an orally effective ligand for the thyroid-stimulating hormone receptor (TSHR) that inhibits the proliferation of MDA-T32 and MDA-T85 cells both in vitro and in vivo, with IC50 values of 0.71 μM and 0.38 μM, respectively. Additionally, it suppresses the metastasis of MDA-T85F1 in mice. NCATS-SM4420 holds potential for research in the field of thyroid cancer.</p>
    Formula:C31H27N3O5
    Colore e forma:Solid
    Peso molecolare:521.56
  • Neflumozide

    CAS:
    Neflumozide (HRP 913) is an orally effective derivative of benzisoxazole, characterized by its potent dopamine antagonist properties and antipsychotic activity. It is utilized in research related to psychiatric disorders.
    Formula:C22H23FN4O2
    Colore e forma:Solid
    Peso molecolare:394.44
  • Nedemelteon

    CAS:
    <p>Nedemelteon is an agonist of the melatonin receptor (melatonin receptor).</p>
    Formula:C15H18N2O2
    Colore e forma:Solid
    Peso molecolare:258.32
  • (Rac)-BI 703704

    CAS:
    (Rac)-BI 703704 is a potent activator of soluble guanylyl cyclase (sGC).
    Formula:C32H37N3O4S
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:559.72
  • Zafirlukast metabolite M1

    CAS:
    <p>Zafirlukast metabolite M1 (compound 15) is an inhibitor used in the treatment of asthma and other allergic pulmonary conditions, effectively antagonizing leukotriene activity.</p>
    Formula:C25H25N3O4S
    Colore e forma:Solid
    Peso molecolare:463.549
  • CVT-5440

    CAS:
    CVT-5440 is a selective, high-affinity (2B) adenosine receptor antagonist with good selectivity.
    Formula:C27H28N6O5
    Colore e forma:Solid
    Peso molecolare:516.55
  • PF-06372222

    CAS:
    <p>PF-06372222: a small-molecule that modulates GCGR and antagonizes GLP-1R, affecting insulin and glucagon.</p>
    Formula:C26H28F3N5O3
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:515.53
  • Fasitibant

    CAS:
    <p>Fasitibant is a potent and selective nonpeptide kinin B2 receptor antagonist.</p>
    Formula:C36H49Cl2N6O6S
    Colore e forma:Solid
    Peso molecolare:764.78