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GPCR/G-Protein

GPCR/G-Protein

GPCR/G-Protein inhibitors are compounds that target G-protein coupled receptors (GPCRs) and associated G-proteins, which play critical roles in transmitting signals from the outside to the inside of cells. These inhibitors are essential for studying the signaling pathways mediated by GPCRs, which are involved in numerous physiological processes, including sensory perception, immune response, and neurotransmission. GPCR inhibitors are also important in drug development, as many therapeutic agents target these receptors. At CymitQuimica, we offer a wide range of high-quality GPCR/G-Protein inhibitors to support your research in pharmacology, cell biology, and related fields.

Subcategories of "GPCR/G-Protein"

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Found 5378 products of "GPCR/G-Protein"

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  • H3R antagonist 2


    <p>Compound 23: H3R antagonist with 170 nM Ki; inhibits AChE, BChE, hMAO B; IC50s: 180, 880, 775 nM; anti-pain, memory boost; crosses BBB. [1]</p>
    Formula:C24H29NO3
    Color and Shape:Solid
    Molecular weight:379.49
  • 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
    Color and Shape:Solid
    Molecular weight:232.32
  • AMG-369

    CAS:
    <p>AMG-369 (AMG 247) is an S1P1/S1P5 dual agonist that delays the development of experimental autoimmune encephalomyelitis in rats.</p>
    Formula:C26H22FN3O2S
    Purity:98.04% - 98.92%
    Color and Shape:Solid
    Molecular weight:459.54
  • (Rac)-BI 703704

    CAS:
    <p>(Rac)-BI 703704 is a potent activator of soluble guanylyl cyclase (sGC).</p>
    Formula:C32H37N3O4S
    Purity:98%
    Color and Shape:Solid
    Molecular weight:559.72
  • LY210073

    CAS:
    <p>LY210073 is an antagonist of the Leukotriene B4 (LTB4) receptor (IC50: 6.2 nM).</p>
    Formula:C30H28O8
    Purity:98%
    Color and Shape:Solid
    Molecular weight:516.54
  • CVT-5440

    CAS:
    <p>CVT-5440 is a selective, high-affinity (2B) adenosine receptor antagonist with good selectivity.</p>
    Formula:C27H28N6O5
    Color and Shape:Solid
    Molecular weight:516.55
  • PAR4 antagonist 3

    CAS:
    <p>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.</p>
    Formula:C22H16FN3O5S
    Molecular weight:453.44
  • Fasitibant

    CAS:
    <p>Fasitibant is a potent and selective nonpeptide kinin B2 receptor antagonist.</p>
    Formula:C36H49Cl2N6O6S
    Color and Shape:Solid
    Molecular weight:764.78
  • 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
    Color and Shape:Solid
    Molecular weight:328.43
  • Tezosentan

    CAS:
    <p>Tezosentan is an antagonist of the endothelin receptor (pA2s: 9.5, 7.7 for ETA and ETB receptors, respectively).</p>
    Formula:C27H27N9O6S
    Purity:98%
    Color and Shape:Solid
    Molecular weight:605.63
  • BAY-899

    CAS:
    <p>BAY-899, oral LH-R antagonist, IC50: 185 nM (hLH), 46 nM (rLH), lowers sex hormones in vivo.</p>
    Formula:C25H19F2N5O2
    Purity:98%
    Color and Shape:Solid
    Molecular weight:459.45
  • 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
    Color and Shape:Solid
    Molecular weight:463.49
  • CCR1 antagonist 11 hydrochloride


    <p>Oral CCR1 antagonist A1B1 targets h/m/rCCR1 (IC50: 0.03/0.58/0.32 μM), potential for treating inflammatory diseases.</p>
    Color and Shape:Solid
  • PF-9404C

    CAS:
    <p>PF-9404C: S-S diastereoisomer, beta-blocker with vasodilation, boosts cyclic GMP in rat aorta cells from 3 to 53 pmol/mg protein.</p>
    Formula:C16H25N3O9
    Purity:98%
    Color and Shape:Solid
    Molecular weight:403.38
  • 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
    Color and Shape:Solid
    Molecular weight:548.869
  • (S)-Praziquantel

    CAS:
    <p>(S)-Praziquantel is the inactive isomer of R-praziquantel.</p>
    Formula:C19H24N2O2
    Color and Shape:Solid
    Molecular weight:312.406
  • Org-6906

    CAS:
    <p>DCB-3503, a tylophorine analog, may treat cancer and suppress immunity by blocking protein synthesis and modulating HSC70's ATPase activity.</p>
    Formula:C13H16ClN
    Purity:98%
    Color and Shape:Solid
    Molecular weight:221.73
  • Cicaprost

    CAS:
    <p>Cicaprost (ZK 96480) is an IP agonist with artery relaxing effects; EC50 is 5.8 nM.</p>
    Formula:C22H30O5
    Color and Shape:Solid
    Molecular weight:374.47
  • SR 140333

    CAS:
    <p>SR 140333 is a NK1 receptor antagonist.</p>
    Formula:C37H45Cl3N2O2
    Purity:98%
    Color and Shape:Solid
    Molecular weight:656.12
  • MF-592

    CAS:
    <p>MF-592: EP4 receptor antagonist, hEP4 IC50 3 nM, hWB IC50 78 nM, great oral PK, rat arthritis ED50 0.1 mg/kg/day, promising for development.</p>
    Formula:C34H33Cl2N3O6S
    Color and Shape:Solid
    Molecular weight:682.61
  • Tebideutorexant

    CAS:
    <p>Tebideutorexant, an orexin-1 receptor antagonist, shows anti-panic effects in rodents and humans, providing a tool for stress response and psychiatric research.</p>
    Formula:C23H16D2F4N4O2
    Purity:98.89%
    Color and Shape:Solid
    Molecular weight:460.42
  • Pexacerfont

    CAS:
    <p>Pexacerfont (BMS-562086) is a selective antagonist of the corticotropin-releasing factor receptor (IC50: 6.1±0.6 nM for the human CRF1 receptor).</p>
    Formula:C18H24N6O
    Purity:99.77%
    Color and Shape:Solid
    Molecular weight:340.42
  • CS-0777

    CAS:
    <p>CS-0777 is a potent, selective, and orally active S1P1 agonist (sphingosine 1-phosphate receptor modulator).</p>
    Formula:C21H31N2O5P
    Color and Shape:Solid
    Molecular weight:422.45
  • SGL5213

    CAS:
    <p>SGL5213 is a potent oral SGLT1 inhibitor (IC50: 29 nM) with potential for treating type 2 diabetes.</p>
    Formula:C37H55N3O8
    Purity:98%
    Color and Shape:Solid
    Molecular weight:669.85
  • Delmadinone acetate

    CAS:
    <p>Delmadinone acetate is an orally active compound used to control estrus and ovulation in both female and male pets. It induces adrenal suppression by inhibiting the pituitary release of ACTH.</p>
    Formula:C23H27ClO4
    Color and Shape:Solid
    Molecular weight:402.911
  • BI-44370

    CAS:
    <p>BI-44370, a CGRP (calcitonin gene-related peptide) receptor antagonist, can be used to treat migraines and other chronic pain.</p>
    Formula:C35H47N5O6
    Color and Shape:Solid
    Molecular weight:633.78
  • Rivenprost

    CAS:
    <p>Rivenprost, selective EP4 agonist (Ki: 0.7 nM), promotes bone growth, osteoblast differentiation, and aids wound healing.</p>
    Formula:C24H34O6S
    Color and Shape:Solid
    Molecular weight:450.59
  • Tofogliflozin

    CAS:
    Tofogliflozin specifically inhibits SGLT2; IC50s are 2.9 nM (human), 14.9 nM (rat), 6.4 nM (mouse).
    Formula:C22H26O6
    Purity:98%
    Color and Shape:Solid
    Molecular weight:386.44
  • LJ-4517


    <p>LJ-4517 is an effective A2AAR antagonist (Ki=18.3 nM). LJ-4517 can effectively replace the binding of [3H] ZM241385 at WT A2AAR.</p>
    Formula:C19H21N5O3S
    Color and Shape:Solid
    Molecular weight:399.47
  • Netupitant metabolite Monohydroxy Netupitant

    CAS:
    Monohydroxy Netupitant is a highly selective antagonist of NK1 receptor, and is Netupitant metabolite.
    Formula:C30H32F6N4O2
    Purity:98%
    Color and Shape:Solid
    Molecular weight:594.59
  • DA-302168S

    CAS:
    <p>DA-302168S is an orally active, selective GLP-1R agonist with an EC50 value of 1.32 nM. It promotes insulin secretion and has a hypoglycemic effect. Additionally, DA-302168S reduces food intake. It primarily activates GLP-1R in humans and monkeys, with minimal effect on GLP-1R in rats, mice, and dogs. DA-302168S can be used for research in type 2 diabetes and obesity.</p>
    Formula:C33H24ClF2N3O5
    Color and Shape:Solid
    Molecular weight:616.011
  • (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
    Color and Shape:Solid
    Molecular weight:534.427
  • HU-308

    CAS:
    <p>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.</p>
    Formula:C27H42O3
    Color and Shape:Solid
    Molecular weight:414.62
  • FK-3657

    CAS:
    <p>FK-3657 is a non-peptide antagonist of bradykinin (BK)-B2 receptor.</p>
    Formula:C30H27Cl2N5O4
    Color and Shape:Solid
    Molecular weight:592.47
  • RF9 hydrochloride


    <p>RF9 hydrochloride is a potent and selective Neuropeptide FF receptor antagonist that acts on hNPFF1R (Ki: 58 nM) and hNPFF2R (Ki: 7 nM).</p>
    Formula:C26H39ClN6O3
    Color and Shape:Solid
    Molecular weight:519.08
  • Histamine H3 antagonist-1

    CAS:
    <p>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].</p>
    Formula:C24H28F3N3O2
    Color and Shape:Solid
    Molecular weight:447.49
  • MK-8825

    CAS:
    <p>MK-8825 is a CGRP receptor antagonist.</p>
    Formula:C31H30F2N6O3
    Color and Shape:Solid
    Molecular weight:572.61
  • CB1/2 agonist 1


    <p>Potent CB1/2 agonist 1; crosses blood-brain barrier; anti-inflammatory, analgesic; for multiple sclerosis research.</p>
    Formula:C21H24BrFN2O2
    Color and Shape:Solid
    Molecular weight:435.33
  • NK-1 Antagonist 1

    CAS:
    <p>NK-1 Antagonist 1 is a NK-1 receptor antagonist.</p>
    Formula:C25H23F6N5O2
    Purity:98%
    Color and Shape:Solid
    Molecular weight:539.47
  • 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
    Purity:98%
    Color and Shape:Solid
    Molecular weight:612.72
  • MRS2179 tetrasodium hydrate


    <p>MRS2179 blocks turkey P2Y1 receptor (Kb 102 nM, pA2 6.99), affects platelet aggregation, and has varying IC50s on P2 receptors.</p>
    Formula:C11H15N5Na4O10P2
    Color and Shape:Solid
    Molecular weight:576.21
  • Cloprostenol

    CAS:
    <p>Cloprostenol is a synthetic prostaglandin and PGF2α analogue used in animals to terminate pregnancy and induce corpus luteum dissolution.</p>
    Formula:C22H29ClO6
    Purity:99.81%
    Color and Shape:Clear Colorless To Light Yellowish Liquid
    Molecular weight:424.92
  • SphK2-IN-2


    <p>SphK2-IN-2 (21g) is a potent and selective inhibitor of SphK2 (IC50: 0.23 μM).</p>
    Formula:C21H25ClN10O
    Color and Shape:Solid
    Molecular weight:468.94
  • RTIOXA-43

    CAS:
    <p>RTIOXA-43 is an OX2R/OX1R (orexin receptor) dual agonist that increases wakefulnesand is commonly used in studies related to narcolepsy and neural signaling.</p>
    Formula:C37H37N5O5S
    Purity:99.17%
    Color and Shape:Solid
    Molecular weight:663.79
  • MDMB-FUBICA

    CAS:
    <p>MDMB-FUBICA is a potent agonist of the cannabinoid receptors and exhibits psychoactive properties. It can be utilized in e-cigarettes.</p>
    Formula:C23H25FN2O3
    Color and Shape:Solid
    Molecular weight:396.455
  • Sulamserod hydrochloride

    CAS:
    <p>Sulamserod hydrochloride is a 5-HT4 receptor antagonist. It is utilized in research related to gastrointestinal disorders.</p>
    Formula:C19H29Cl2N3O5S
    Color and Shape:Solid
    Molecular weight:482.42
  • SEP-363856 mesylate

    CAS:
    <p>SEP-363856 (SEP-856) mesylate is an orally active compound that acts as an agonist for both TAAR1 and 5-HT1A receptors. This compound exhibits antipsychotic activity in the central nervous system and has potential for the study of schizophrenia.</p>
    Formula:C10H17NO4S2
    Color and Shape:Solid
    Molecular weight:279.38
  • Dopamine D4 receptor ligand 3

    CAS:
    <p>Dopamine D4 receptor ligand 3 (Compound 16) functions as a dopamine D4 receptor (D4R) antagonist with a pKi of 8.86. In HEK-293T cells, it shows pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors, respectively. This compound inhibits the activity of human glioma cell lines U87 MG, T98G, and U251 MG, and it induces ROS production and mitochondrial dysfunction in these glioma cells.</p>
    Formula:C28H31N3O5
    Color and Shape:Solid
    Molecular weight:489.56
  • 2,3-dinor-11β-Prostaglandin F2α

    CAS:
    <p>2,3-dinor-11β-Prostaglandin F2α (2,3-dinor-11β-PGF2α) was recovered from the urine of both normal monkeys and humans when infused with radiolabeled PGD2, where</p>
    Formula:C18H30O5
    Color and Shape:Solid
    Molecular weight:326.43
  • SGLT inhibitor-1

    CAS:
    <p>SGLT inhibitor-1 is a potentsodium glucose co-transporter proteins (SGLTs) dual inhibitor(hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively).</p>
    Formula:C24H27FO8
    Purity:98%
    Color and Shape:Solid
    Molecular weight:462.46