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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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  • (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
  • Serlopitant

    CAS:
    <p>Serlopitant is a selective antagonist of Neurokinin-1 (NK-1) receptor.</p>
    Formula:C29H28F7NO2
    Color and Shape:Solid
    Molecular weight:555.53
  • 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
  • GAT564


    <p>GAT564, an allosteric CB1R modulator, shows EC50s of 87 nM (cAMP) &amp; 320 nM (β-arrestin2) and lowers IOP effectively in glaucoma mice.</p>
    Formula:C20H16N2O2S
    Color and Shape:Solid
    Molecular weight:348.42
  • H3R antagonist 5

    CAS:
    <p>H3R antagonist 5 (Compound 1b) is a selective inverse agonist of the histamine H3 receptor that can penetrate the blood-brain barrier, with an IC50 of 0.54 nM. It is applicable for research related to the central nervous system.</p>
    Formula:C23H32N2O4
    Color and Shape:Solid
    Molecular weight:400.511
  • 5-HT1A modulator 4

    CAS:
    <p>5-HT1A modulator 4 (Compound 1) is a ligand for the 5-HT receptor, with Ki values of 2.18 μM for 5-HT1A and 19.7 μM for 5-HT2A.</p>
    Formula:C9H14N4
    Color and Shape:Solid
    Molecular weight:178.234
  • Metrazoline

    CAS:
    <p>Metrazoline (o-Methyl-tracizoline) acts as a ligand for adrenergic receptors (low affinity) and imidazoline I2 receptors.</p>
    Formula:C14H16N2O4
    Color and Shape:Solid
    Molecular weight:276.288
  • SB 224289

    CAS:
    <p>SB 224289: selective 5-HT1B antagonist, pKi 8.2, 60x selectivity, effective orally.</p>
    Formula:C32H32N4O3
    Purity:98%
    Color and Shape:Solid
    Molecular weight:520.62
  • 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
  • RS 12254

    CAS:
    <p>RS 12254 is a dopamine agonist and antihypertensive agent.</p>
    Formula:C28H40N2O4
    Purity:98%
    Color and Shape:Solid
    Molecular weight:468.63
  • 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
    Purity:99.36%
    Color and Shape:White Crystalline Solid
    Molecular weight:573.68
  • CM699

    CAS:
    <p>CM699 is an effective dual inhibitor of the dopamine transporter (DAT) and Sigma receptor (σR), with IC50 values of 311 nM and 14.1 nM, respectively.</p>
    Formula:C24H29N3O2
    Color and Shape:Solid
    Molecular weight:391.51
  • RBM10-8

    CAS:
    <p>RBM10-8 irreversibly inhibits human sphingosine-1- phosphate lyase (hS1PL) while behaving also as an enzyme substrate.</p>
    Formula:C17H36NO5P
    Color and Shape:Solid
    Molecular weight:365.45
  • Nolpitantium besilate

    CAS:
    <p>Nolpitantium besilate is a neurokinin-1 receptor antagonist.</p>
    Formula:C43H50Cl2N2O5S
    Color and Shape:Solid
    Molecular weight:777.84
  • Lp(a)-IN-8

    CAS:
    <p>LPA2 antagonist 3 (compound 15) serves as an Lp(a) antagonist. Lp(a) is a pathogenic risk factor for atherosclerotic cardiovascular disease (ASCVD).</p>
    Formula:C21H40Cl2N4O5
    Color and Shape:Solid
    Molecular weight:499.472
  • S1PR1 agonist 1

    CAS:
    <p>S1PR1 agonist 1 is a potent agonist of S1PR1. S1PR1 agonist 1 has potential in autoimmune diseases.</p>
    Formula:C29H30N4O4
    Color and Shape:Solid
    Molecular weight:498.57
  • Pareptide monohydrochloride

    CAS:
    <p>Pareptide monohydrochloride is a metabolically stable analog of melatonin inhibitor (MIF).</p>
    Formula:C14H27ClN4O3
    Purity:98%
    Color and Shape:Solid
    Molecular weight:334.84
  • ATX inhibitor 27

    CAS:
    <p>ATX inhibitor 27 (Compound 31) is an ATX inhibitor. It demonstrates IC50 values of 13 nM against human autotaxin (hATX) and 23 nM against lysophosphatidylcholine (LPC). By inhibiting the ATX enzyme, ATX inhibitor 27 reduces LPA levels in the body. This compound is applicable in research related to ATX-LPA-associated conditions such as inflammation, neurodegenerative disorders, and cancer.</p>
    Formula:C26H26ClN5O3
    Color and Shape:Solid
    Molecular weight:491.97
  • BD-1047

    CAS:
    <p>BD-1047 is a selective functional antagonist of sigma receptors. It can alleviate climbing behavior induced by Apomorphine and head twitching caused by Phencyclidine.</p>
    Formula:C13H20Cl2N2
    Color and Shape:Solid
    Molecular weight:275.217
  • Iralukast (CGP 45715A)

    CAS:
    <p>Iralukast is a cysteinyl-leukotriene antagonist (CysLT) with a pKi of 7.8 for CysLT1.</p>
    Formula:C38H37F3O8S
    Color and Shape:Solid
    Molecular weight:710.76
  • MDA7

    CAS:
    <p>MDA7 is a selective agonist of the cannabinoid receptor 2 (CB2), demonstrating an EC50 of 128 nM in human CB2 receptors and 67.4 nM in rat CB2 receptors. The compound exhibits good affinity for CB2 receptors, with Ki values of 422 nM for humans and 238 nM for rats. In rat models, MDA7 shows analgesic activity.</p>
    Formula:C22H25NO2
    Color and Shape:Solid
    Molecular weight:335.439
  • COX-2-IN-6

    CAS:
    <p>COX-2-IN-6: Potent, selective COX-2 inhibitor; oral; IC50 0.84μM, Ki 69nM; blocks PGE2 synthesis; prevents colorectal cancer.</p>
    Formula:C20H27NO6S
    Purity:99.29% - 99.69%
    Color and Shape:Soild
    Molecular weight:409.5
  • SB 258741 hydrochloride


    <p>SB 258741 hydrochloride is a potent antagonist of the 5-HT 7 receptor, designed specifically for studying schizophrenia [1].</p>
    Formula:C19H31ClN2O2S
    Color and Shape:Solid
    Molecular weight:386.98
  • GLP-1R agonist 8

    CAS:
    <p>GLP-1R agonist 8 is a potent agonist of GLP-1R (EC50 &lt; 2 nM).</p>
    Formula:C33H32N4O5
    Color and Shape:Solid
    Molecular weight:564.63
  • S1P1 agonist 4

    CAS:
    <p>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, indicating</p>
    Formula:C24H31NO3
    Color and Shape:Solid
    Molecular weight:381.51
  • ONO-9780307

    CAS:
    <p>ONO-9780307 is a specific antagonist of LPA1 (lysophosphatidic acid receptor 1) (IC50: 2.7 nM).</p>
    Formula:C30H35NO7
    Color and Shape:Solid
    Molecular weight:521.6
  • RU 52583

    CAS:
    <p>RU 52583 is an alpha 2-adrenergic receptor antagonist.</p>
    Formula:C18H20N2
    Purity:98%
    Color and Shape:Solid
    Molecular weight:264.36
  • CHF-6366

    CAS:
    <p>CHF-6366: M3 antagonist &amp; β2 agonist (pKi 10.4/11.4), mild Ca channel blocker, used in COPD study.</p>
    Formula:C42H48N6O8
    Color and Shape:Solid
    Molecular weight:764.87
  • Anthrotainin

    CAS:
    Anthrotainin is a tetracyclic compound that acts as an inhibitor of the binding of P substance (substance P), with an IC50 of 3 μM.
    Formula:C20H17NO9
    Color and Shape:Solid
    Molecular weight:415.35
  • M1069


    <p>M1069 is an oral A2A/A2B receptor antagonist, 100x more selective over A1/A3, with antitumor properties by blocking adenosine's immunosuppressive effects.</p>
    Formula:C25H30N4O8S
    Color and Shape:Solid
    Molecular weight:546.59
  • 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
  • WIN 62577

    CAS:
    <p>WIN 62577 is a species-selective tachykinin NK1 receptor antagonist and also serves as an allosteric enhancer with micromolar potency at M3 receptors. Additionally, WIN 62577 demonstrates potent antiviral activity against SARS-CoV-2.</p>
    Formula:C29H31N3O
    Color and Shape:Solid
    Molecular weight:437.576
  • Atumelnant

    CAS:
    Atumelnant (CRN04894) is an MC2R antagonist used in the study of congenital adrenocortical hyperplasia (CAH) and Cushing's disease (CD).
    Formula:C33H42F3N5O3
    Purity:98.41%
    Color and Shape:Solid
    Molecular weight:613.71
  • OP-2507

    CAS:
    <p>OP-2507, a prostacyclin agonist, is used potentially for the treatment of hepatic insufficiency and hypertension.</p>
    Formula:C25H41NO4
    Purity:98%
    Color and Shape:Solid
    Molecular weight:419.6
  • Ro4368554

    CAS:
    <p>Ro4368554 is a selective 5-HT6 antagonist capable of crossing the blood-brain barrier. It can reverse memory deficits caused by scopolamine and tryptophan depletion. Ro4368554 is applicable for research related to memory impairments.</p>
    Formula:C19H21N3O2S
    Color and Shape:Solid
    Molecular weight:355.454
  • SGLT1/2-IN-1

    CAS:
    <p>SGLT1/2-IN-1 is a dual SGLT1/SGLT2 inhibitor.</p>
    Formula:C25H28O8
    Color and Shape:Solid
    Molecular weight:456.48
  • H1R ligand-1

    CAS:
    <p>H1R ligand-1 (Compound fragment 1) is a high-affinity ligand for the human histamine H1 receptor (H1R). It can serve as a scaffold for synthesizing a series of derivatives to investigate H1R binding kinetics.</p>
    Formula:C19H23NO
    Color and Shape:Solid
    Molecular weight:281.392
  • AM8936


    <p>AM8936: potent CB1 agonist, EC50 rCB1=8.6nM/hCB1=1.4nM, Ki rat CB1=0.55nM; potential for CNS, metabolic, pain, glaucoma research.</p>
    Formula:C25H33NO3
    Color and Shape:Solid
    Molecular weight:395.53
  • 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
  • PF-00446687

    CAS:
    PF-00446687 is a selective agonist of melanocortin-4 receptor (MC4R) (EC50 of 12 ± 1 nM).
    Formula:C28H36F2N2O2
    Purity:98%
    Color and Shape:Solid
    Molecular weight:470.59
  • Merigolix

    CAS:
    <p>Merigolix is a potent gonadotrophin releasing hormone (GnRH) antagonist .</p>
    Formula:C36H35F7N4O6
    Color and Shape:Solid
    Molecular weight:752.68
  • Vibegron

    CAS:
    <p>Vibegron (MK-4618) is an effective and selective Beta 3 adrenergic receptor agonist, used to treat overactive bladder (OAB).</p>
    Formula:C26H28N4O3
    Color and Shape:Solid
    Molecular weight:444.53
  • 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
  • AChE-IN-5


    <p>AChE-IN-5: oral, crosses blood-brain barrier, targets AChE/5-HT1A/SERT, potent with 2.29 nM IC50.</p>
    Formula:C38H45N5O
    Color and Shape:Solid
    Molecular weight:587.8
  • L 668750

    CAS:
    <p>L 668750 is an inhibitor of platelet-activating factor.</p>
    Formula:C25H34O9S
    Purity:98%
    Color and Shape:Solid
    Molecular weight:510.6
  • 5-IAI hydrochloride

    CAS:
    <p>5-IAI hydrochloride is a psychoactive analog of para-iodoamphetamine. 5-IAI hydrochloride significantly reduces serotonin uptake sites and hippocampal serotonin levels in rats.</p>
    Formula:C9H11ClIN
    Color and Shape:Solid
    Molecular weight:295.548
  • SSTR4 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>
    Formula:C19H26N4O
    Color and Shape:Solid
    Molecular weight:326.44
  • RS 61756-007

    CAS:
    <p>RS 61756-007 is a selective thromboxane receptor (TP) agonist.</p>
    Formula:C23H28O5
    Purity:98%
    Color and Shape:Solid
    Molecular weight:384.47
  • CCG258208

    CAS:
    <p>GRKs-IN-1 has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).</p>
    Formula:C24H25FN4O4
    Purity:98%
    Color and Shape:Solid
    Molecular weight:452.48
  • LPA2 antagonist 6

    CAS:
    <p>LPA2 antagonist 6 (example 2) acts as an antagonist of Lp(a). It inhibits the formation of Lp(a) with an IC50 value of 2.33 nM, making it useful for cardiovascular disease research.</p>
    Formula:C26H34Cl2N2O6
    Color and Shape:Solid
    Molecular weight:541.464