
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"
- 5-HT Receptor(942 products)
- Adenosine Receptor(242 products)
- Adrenergic Receptor(2,949 products)
- Bombesin Receptor(30 products)
- Bradykinin Receptor(59 products)
- CXCR(149 products)
- CaSR(32 products)
- Cannabinoid Receptor(195 products)
- Dopamine Receptor(410 products)
- Endothelin Receptor(75 products)
- GNRH Receptor(73 products)
- GPCR19(31 products)
- GRK(32 products)
- GTPase(21 products)
- Glucagon Receptor(166 products)
- Hedgehog/Smoothened(45 products)
- Histamine Receptor(359 products)
- LPA Receptor(21 products)
- Melatonin Receptor(24 products)
- OX Receptor(40 products)
- Opioid Receptor(298 products)
- PAFR(11 products)
- PKA(49 products)
- S1P Receptor(17 products)
- SGLT(30 products)
- Sigma receptor(46 products)
Show 18 more subcategories
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:C32H37N3O4SPurity:98%Color and Shape:SolidMolecular weight:559.72Serlopitant
CAS:<p>Serlopitant is a selective antagonist of Neurokinin-1 (NK-1) receptor.</p>Formula:C29H28F7NO2Color and Shape:SolidMolecular weight:555.53Dopamine 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:C28H31N3O5Color and Shape:SolidMolecular weight:489.56GAT564
<p>GAT564, an allosteric CB1R modulator, shows EC50s of 87 nM (cAMP) & 320 nM (β-arrestin2) and lowers IOP effectively in glaucoma mice.</p>Formula:C20H16N2O2SColor and Shape:SolidMolecular weight:348.42H3R 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:C23H32N2O4Color and Shape:SolidMolecular weight:400.5115-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:C9H14N4Color and Shape:SolidMolecular weight:178.234Metrazoline
CAS:<p>Metrazoline (o-Methyl-tracizoline) acts as a ligand for adrenergic receptors (low affinity) and imidazoline I2 receptors.</p>Formula:C14H16N2O4Color and Shape:SolidMolecular weight:276.288SB 224289
CAS:<p>SB 224289: selective 5-HT1B antagonist, pKi 8.2, 60x selectivity, effective orally.</p>Formula:C32H32N4O3Purity:98%Color and Shape:SolidMolecular weight:520.62CVT-5440
CAS:<p>CVT-5440 is a selective, high-affinity (2B) adenosine receptor antagonist with good selectivity.</p>Formula:C27H28N6O5Color and Shape:SolidMolecular weight:516.55RS 12254
CAS:<p>RS 12254 is a dopamine agonist and antihypertensive agent.</p>Formula:C28H40N2O4Purity:98%Color and Shape:SolidMolecular weight:468.63IRL 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:C36H35N3O4Purity:99.36%Color and Shape:White Crystalline SolidMolecular weight:573.68CM699
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:C24H29N3O2Color and Shape:SolidMolecular weight:391.51RBM10-8
CAS:<p>RBM10-8 irreversibly inhibits human sphingosine-1- phosphate lyase (hS1PL) while behaving also as an enzyme substrate.</p>Formula:C17H36NO5PColor and Shape:SolidMolecular weight:365.45Nolpitantium besilate
CAS:<p>Nolpitantium besilate is a neurokinin-1 receptor antagonist.</p>Formula:C43H50Cl2N2O5SColor and Shape:SolidMolecular weight:777.84Lp(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:C21H40Cl2N4O5Color and Shape:SolidMolecular weight:499.472S1PR1 agonist 1
CAS:<p>S1PR1 agonist 1 is a potent agonist of S1PR1. S1PR1 agonist 1 has potential in autoimmune diseases.</p>Formula:C29H30N4O4Color and Shape:SolidMolecular weight:498.57Pareptide monohydrochloride
CAS:<p>Pareptide monohydrochloride is a metabolically stable analog of melatonin inhibitor (MIF).</p>Formula:C14H27ClN4O3Purity:98%Color and Shape:SolidMolecular weight:334.84ATX 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:C26H26ClN5O3Color and Shape:SolidMolecular weight:491.97BD-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:C13H20Cl2N2Color and Shape:SolidMolecular weight:275.217Iralukast (CGP 45715A)
CAS:<p>Iralukast is a cysteinyl-leukotriene antagonist (CysLT) with a pKi of 7.8 for CysLT1.</p>Formula:C38H37F3O8SColor and Shape:SolidMolecular weight:710.76MDA7
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:C22H25NO2Color and Shape:SolidMolecular weight:335.439COX-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:C20H27NO6SPurity:99.29% - 99.69%Color and Shape:SoildMolecular weight:409.5SB 258741 hydrochloride
<p>SB 258741 hydrochloride is a potent antagonist of the 5-HT 7 receptor, designed specifically for studying schizophrenia [1].</p>Formula:C19H31ClN2O2SColor and Shape:SolidMolecular weight:386.98GLP-1R agonist 8
CAS:<p>GLP-1R agonist 8 is a potent agonist of GLP-1R (EC50 < 2 nM).</p>Formula:C33H32N4O5Color and Shape:SolidMolecular weight:564.63S1P1 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:C24H31NO3Color and Shape:SolidMolecular weight:381.51ONO-9780307
CAS:<p>ONO-9780307 is a specific antagonist of LPA1 (lysophosphatidic acid receptor 1) (IC50: 2.7 nM).</p>Formula:C30H35NO7Color and Shape:SolidMolecular weight:521.6RU 52583
CAS:<p>RU 52583 is an alpha 2-adrenergic receptor antagonist.</p>Formula:C18H20N2Purity:98%Color and Shape:SolidMolecular weight:264.36CHF-6366
CAS:<p>CHF-6366: M3 antagonist & β2 agonist (pKi 10.4/11.4), mild Ca channel blocker, used in COPD study.</p>Formula:C42H48N6O8Color and Shape:SolidMolecular weight:764.87Anthrotainin
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:C20H17NO9Color and Shape:SolidMolecular weight:415.35M1069
<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:C25H30N4O8SColor and Shape:SolidMolecular weight:546.59HU-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:C27H42O3Color and Shape:SolidMolecular weight:414.62WIN 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:C29H31N3OColor and Shape:SolidMolecular weight:437.576Atumelnant
CAS:Atumelnant (CRN04894) is an MC2R antagonist used in the study of congenital adrenocortical hyperplasia (CAH) and Cushing's disease (CD).Formula:C33H42F3N5O3Purity:98.41%Color and Shape:SolidMolecular weight:613.71OP-2507
CAS:<p>OP-2507, a prostacyclin agonist, is used potentially for the treatment of hepatic insufficiency and hypertension.</p>Formula:C25H41NO4Purity:98%Color and Shape:SolidMolecular weight:419.6Ro4368554
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:C19H21N3O2SColor and Shape:SolidMolecular weight:355.454SGLT1/2-IN-1
CAS:<p>SGLT1/2-IN-1 is a dual SGLT1/SGLT2 inhibitor.</p>Formula:C25H28O8Color and Shape:SolidMolecular weight:456.48H1R 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:C19H23NOColor and Shape:SolidMolecular weight:281.392AM8936
<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:C25H33NO3Color and Shape:SolidMolecular weight:395.53PD 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:C35H40N4O6Purity:98%Color and Shape:SolidMolecular weight:612.72PF-00446687
CAS:PF-00446687 is a selective agonist of melanocortin-4 receptor (MC4R) (EC50 of 12 ± 1 nM).Formula:C28H36F2N2O2Purity:98%Color and Shape:SolidMolecular weight:470.59Merigolix
CAS:<p>Merigolix is a potent gonadotrophin releasing hormone (GnRH) antagonist .</p>Formula:C36H35F7N4O6Color and Shape:SolidMolecular weight:752.68Vibegron
CAS:<p>Vibegron (MK-4618) is an effective and selective Beta 3 adrenergic receptor agonist, used to treat overactive bladder (OAB).</p>Formula:C26H28N4O3Color and Shape:SolidMolecular weight:444.53Org-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:C13H16ClNPurity:98%Color and Shape:SolidMolecular weight:221.73AChE-IN-5
<p>AChE-IN-5: oral, crosses blood-brain barrier, targets AChE/5-HT1A/SERT, potent with 2.29 nM IC50.</p>Formula:C38H45N5OColor and Shape:SolidMolecular weight:587.8L 668750
CAS:<p>L 668750 is an inhibitor of platelet-activating factor.</p>Formula:C25H34O9SPurity:98%Color and Shape:SolidMolecular weight:510.65-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:C9H11ClINColor and Shape:SolidMolecular weight:295.548SSTR4 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:C19H26N4OColor and Shape:SolidMolecular weight:326.44RS 61756-007
CAS:<p>RS 61756-007 is a selective thromboxane receptor (TP) agonist.</p>Formula:C23H28O5Purity:98%Color and Shape:SolidMolecular weight:384.47CCG258208
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:C24H25FN4O4Purity:98%Color and Shape:SolidMolecular weight:452.48LPA2 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:C26H34Cl2N2O6Color and Shape:SolidMolecular weight:541.464

