GPCR/G-Protein

SSR-241586: Neurokinin antagonist, treats depression, schizophrenia, urinary issues, emesis, IBS.

Atumelnant (CRN04894) is an MC2R antagonist used in the study of congenital adrenocortical hyperplasia (CAH) and Cushing's disease (CD).

<p>GPR27 agonist-1 (compound I) is a selective agonist for GPR27 with a pEC50 value of 6.34.</p>

5-HT2A and 2C receptor antagonist

<p>Substituted piperidines-1 can promote the release of growth hormone in humans and animals.</p>

<p>Alixorexton is an agonist of the orexin-2 receptor (orexin-2 receptor) and is utilized in obesity research.</p>

<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>

Selective oral S1P1 agonist 5 inhibits lymphocyte drainage, potential for MS research.

<p>Compound 6f is a potent, selective 5-HT1A receptor blocker (Ki: 35 nM), useful in CNS disorder research.</p>

BW A868C is a potent, selective PGD2 antagonist and a BW245C analogue, inert to other prostaglandin receptors.

<p>Bometolol Hydrochloride is a beta-adrenergic blocking compound used for the treatment of cardiovascular disease.</p>

<p>AFP-07 is a highly selective and potent agonist. It was used for the prostacyclin receptor.</p>

<p>Methacycline, a tetracycline antibiotic, inhibits bacterial protein synthesis and effectively suppresses epithelial-mesenchymal transition (EMT). It blocks EMT in vitro and inhibits fibrogenesis in vivo without directly affecting the TGF-β1Smad signaling pathway. As an antimicrobial agent, Methacycline holds potential for research in pulmonary fibrosis.</p>

MK-3207 is a potent, oral CGRP receptor antagonist with high selectivity for human and monkey receptors, inhibiting blood flow in vivo.

<p>L-654284 is an α2-adrenergic receptor antagonist characterized by its notable selectivity. It competes with 3H-clonidine and 3H-rauwolscine for binding in vitro, exhibiting Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 effectively blocks the pre-ejaculatory effects of clonidine in isolated rat vas deferens, with a pA2 value of 9.1. The compound demonstrates significant selectivity for α2 over α1 adrenergic receptors, with a Ki value of 110 nM against 3H-prazosin binding. In vivo, L-654284 significantly increases the turnover of norepinephrine in the rat cerebral cortex, indicating its activity in blocking α2-adrenergic receptors within the central nervous system.</p>

Tixanox sodium effectively blocks histamine release in the lungs triggered by anti-IgE. It has also been demonstrated that when administered orally, Tixanox sodium can successfully counteract exercise-induced asthma.

BRD50837 is a potent and selective inhibitor of Sonic Hedgehog (Shh).

<p>TGR5 Receptor Agonist 3 is a GPBAR1 agonist with EC50 of 16.4 nM (hTGR5) &amp; 209 nM (mTGR5), ensures gallbladder safety and reduces filling.</p>

<p>BRL-37344 is a selective β3-adrenergic receptor agonist. It significantly reduces the body weight of obese mice.</p>

Y1 receptor antagonist 1 is an antagonist of neuropeptide Y1 receptor.

<p>K-14585 blocks PAR(2), reduces NFkappaB activity, and IL-8 response, but alone can boost IL-8.</p>

<p>L-365260 hemihydrate: selective oral CCK-B/gastrin blocker, Ki=1.9/2.0 nM, competes with guinea pig receptors.</p>

KAG-308: selective EP4 agonist; Ki: 2.57 nM, EC50: 17 nM; suppresses colitis, promotes mucosal healing, inhibits TNF-α.

<p>LTF4, made in vitro from LTE4 with enzymes, contracts vascular muscle weakly; potency is LTD4 &gt; LTC4 &gt; LTE4 &gt;&gt; LTF4.</p>

<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>

CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg

<p>Potent, selective D4R antagonist; IC50 = 6.87 µM; potential in Parkinson’s disease research.</p>

Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor selective (Ki=2.16 nM) or multi-targeting dual ligand that shows potential effects in CNS disorders.

(E/Z)-Ozagrel (sodium) [(E/Z)-OKY-046 (sodium)] is a mixture of the EZ isomers of Ozagrel (sodium). It acts as a thromboxane A2 (TXA2) synthase inhibitor. As an antiplatelet agent, Ozagrel (sodium) selectively inhibits human platelet aggregation, with an IC50 of 53.12 μM.

<p>SB-423562 is a calcium-sensing receptor (CaSR) antagonist and can be used in studies about osteoporosis.</p>

<p>Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist.Cost-effective and quality-assured.</p>

Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).

<p>PF-07258669 is a selective melanocortin 4 receptor (MC4) antagonist used in the study of cachexia and loss of appetite.</p>

<p>AZD-5672 is an antagonist of CCR5 with an IC50 of 0.32 nM.</p>

<p>LSN3318839 is a potent and orally available glucagon-like peptide-1 receptor (GLP-1R) modulator.LSN3318839 enhances GLP-1R G-protein-coupled signaling and can</p>

<p>SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.</p>

<p>AZD5462 is a potent orally available relaxin receptor RXFP1 agonist for the study of heart failure and cancer.</p>

<p>BMS-986141(UDM-003183) is a selective and potent protease-activated receptor-4 (PAR-4) antagonist with oral activity and an IC50 value of 0.4 nM.BMS-98614</p>

Vofopitant dihydrochloride (GR 205171A) is a tachykinin NK1 receptor antagonist and a potential compound for the treatment of pathologic vomiting.

<p>BQ-788 is an ETB receptor antagonist with potential hypertensive activity that inhibits exogenous ET-1-induced elevation of coronary perfusion pressure.</p>

<p>Treprostinil diethanolamine (UT-15C) is a potent agonist of EP2, DP1 and IP, with values of 3.6, 4.4, 32.1, 212, 826, 2505 and 4680 nM for EP2, DP1, IP, EP1,</p>

<p>Rolapitant HCl is a potent NK1 antagonist, non-CYP3A4 interactive, with anti-emetic effects and a Ki of 0.66 nM.</p>

ML-00253764 hydrochloride is an antagonist of nonpeptidic melanocortin receptor 4 (MC4R) (Ki and IC50 of 0.16 µM and 0.103 µM, respectively).

BIBP3226 TFA is an effective and selective antagonist of neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptor (Kis: 1.1, 79, and 108 nM for rNPY Y1, hNPFF2, and rNPFF).

<p>(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial the 5-HT1A receptor agonist.</p>

SR 146131 is a potent and selective agonist of the nonpeptide receptor.

HOKU-81is a new bronchodilator and is one of the metabolites of tulobuterol.

CYM 9484 is a selective and potent neuropeptide Y (NPY) Y2 receptor antagonist with an IC50 value of 19 nM.

<p>Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand [125I-ICYP] to [5HT1B-serotonergic] receptor sites. It is an antihypertensive agent.</p>

<p>SHA 68 is a potent and selective non-peptide antagonist of neuropeptide S receptor (NPSR) with IC50 values of 22.0 nM for NPSR Asn107 and 23.8 nM for NPSR Ile107.</p>

JMV 2959 is an antagonist of growth hormone secretagogue receptor type 1a (GHS-R1a) (IC50: 32 nM).

<p>Protease-Activated Receptor-4 (PAR4) is a proteinase-activated receptor-4 agonist used in antiplatelet therapy.</p>

7-Desmethyl-agomelatine, a metabolite of Agomelatine, exhibits lower activity than Agomelatine, which functions as a melatonergic (MT1 and MT2) agonist and 5-HT2C antagonist.

Beraprost sodium is a stable and orally active prodrug of PGI2.

<p>ML-290 is an effective relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes. It shows an EC50 of 94 nM.</p>

<p>Pumosetrag Hydrochloride is an orally available 5-HT3 partial agonist. It is developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.</p>

SB-399885 hydrochloride is an antagonist of 5-HT6 receptor.

<p>1-Oleoyl Lysophosphatidic Acid (1-Oleoyl LPA) is a biologically active phospholipid that can be used to study cancer and atherosclerosis.</p>

<p>Patecibart is a humanized immunoglobulin G4-kappa monoclonal antibody that functions as an antagonist to the endothelin receptor A (EDNRA).</p>

<p>GSK-3050002 (HGS-1035) is a humanized IgG1 antibody that targets and binds to CCL20. It holds potential for inflammation research. For isotype control, refer to Human IgG1 kappa, Isotype Control.</p>

TAK-448 (MVT-602), a potent KISS1R agonist, IC50: 460 pM, EC50: 632 pM, trialed for Prostate Cancer and Hypogonadism.

<p>Picumeterol(GR 114297A) is a potent and selective β2 adrenergic receptor agonist. In vitro and in vivo trials, Picumeterol produced long-lasting airway smooth muscle relaxation. Picumeterol is a pure R enantiomer that can be used to improve lung function and reduce airway hyperreactivity in patients with asthma.</p>

<p>3-Hydroxybenzylamine is a useful organic compound for research related to life sciences. The catalog number is T124305 and the CAS number is 73604-31-6.</p>

<p>Dapitant, a non-peptide, selective antagonist of human NKI receptors, is representative of the 7,7,4-triarylperhydroisoindol-4-ols.</p>

<p>Desmethyl cariprazine is a Cariprazine active metabolite. Cariprazine, an antipsychotic drug candidate, shows a high affinity for the D3 (Ki: 0.085 nM) and D2 (Ki: 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM).</p>

BRL 15572 is a useful organic compound for research related to life sciences. The catalog number is T64501 and the CAS number is 734517-40-9.

<p>Propiram fumarate HClis an orally available Opioid receptors agonist with analgesic activity for the study of musculoskeletal pain.</p>

<p>CRTh2 antagonist 3, a potent molecule, activates PDK1 (EC50=2μM, Kd=8.4μM) and may cause cardiovascular inflammation.</p>

BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with a Ki of 1 nM for human CCR1, exhibiting 250-fold selectivity over CCR2, CCR5, and CXCR4.

4-Hydroxypropranolol hydrochloride is an active metabolite of Propranolol, with a potency comparable to Propranolol. It inhibits β1- and β2-adrenergic receptors (pA2s: 8.24 and 8.26).

<p>Vornorexant (ORN-0829; TS-142) is a potent dual OX1R and OX2R antagonist with IC50 values of 1.05 nM and 1.27 nM, respectively. It exhibits potent sleep-promoting effects in vivo and can be used for insomnia treatment research.</p>

<p>Goserelin acetate （ICI-118630 acetate） is a naturally occurring decapeptide, a GnRH (gonadotropin releasing hormone) agonist that reduces the production of sex hormones (testosterone and estrogen) for the treatment of prostate cancer, breast cancer and endometriosis.</p>

<p>(Rac)-Zevaquenabant ((Rac)-MRI-1867, compound 6b) is a potent and selective antagonist of cannabinoid receptor type 1 (CB1R) and inducible nitric oxide synthase (iNOS), with a binding affinity (Ki) of 5.7 nM for CB1R. It holds promise as an investigative tool in liver fibrosis research due to these characteristics.</p>

<p>Anti-GLP1R Antibody is a human antibody expressed in CHO cells, targeting GLP1R. For isotype controls, refer to Human IgG1 kappa, Isotype Control.</p>

Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors, with IC50 values of 6.5 nM for rat 5-HT 1A, 0.1 nM for human 5-HT 1A, 15.1 nM for rat D 2, 17 nM for human D 2, 6.8 nM for human D 3, and 2.4 nM for human D 4.2.

<p>R(-)-alpha-Methylhistamine 2HCl is an effective and selective agonist of the H3 histamine receptor.</p>

6-Chloro-5-(2-chloroethyl)indolin-2-one is a useful organic compound for research related to life sciences. The catalog number is T64862 and the CAS number is 118289-55-7.

1-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-yl)ethanol is a useful organic compound for research related to life sciences. The catalog number is T65156 and the CAS number is 24155-42-8.

SKF 89748 is an agonists of alpha 1-adrenoceptor.

TAK-683: a full KISS1R agonist, IC50=170 pM; a nonapeptide metastin analog with human EC50=0.96 nM, rat EC50=1.6 nM.

4-Hydroxyatomoxetine, an active metabolite of Atomoxetine, is metabolized by CYP2D6. Atomoxetine is a noradrenaline reuptake inhibitor.

<p>Amelubant (BIIL 284) is a prodrug of active metabolites BIIL 260 and BIIL 315 with anti-inflammatory activity[1]. It is a potent, oral, long-acting LTB4 receptor antagonist that negligibly binds to the LTB4 receptor, exhibiting Kis of 221 nM and 230 nM in vital cells and membranes.</p>

<p>Canagliflozin D4 is a deuterium-labeled Canagliflozin. Canagliflozin is an SGLT2 inhibitor.</p>

<p>AM-2232 (UNII-40KCH8YIKP) is a potent and unselective agonist of the cannabinoid receptors.</p>

2-Methyl-5-HT hydrochloride (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist with anti-depressive-like effects.

<p>Pamoic acid is the orphan G protein-coupled receptor GPR35 agonist. Pamoic acid activates ERK and beta-arrestin2 and causes antinociceptive activity.</p>

<p>Neurokinin antagonist 1 is a potent is a neuropeptide antagonist that can be used to study neurological disorders.</p>

MEN11467 is a novel, orally available, potent and selective peptidomimetic tachykinin NK 1 receptor antagonist for the study of acute colon cancer.

Imetit dihydrobromide is a high affinity and effective agonist of histamine H3 and H4 receptors (Ki: 0.3 and 2.7 nM). Imetit mimics the histamine effect in triggering a shape change in eosinophils (EC50: 25 nM).

GR 218,231 is a selective antagonist of D3 dopamine receptor.

Flumexadol is a selective 5-HT2C receptor agonist with an affinity (Ki) of 25 nM for the (+)-enantiomer and exhibits 40-fold selectivity over the 5-HT2A receptor. It is an orally active, non-narcotic analgesic.

SB251023 is an agonist of β3-adrenoceptor.

<p>Compound I (S1P1 agonist 6) is an S1P1 agonist that mitigates autoimmune activity by inhibiting lymphocyte trafficking and has potential as an immunosuppressive</p>

<p>AEF0117 is a signaling inhibitor of CB1-SSi that inhibits cannabinoid self-administration and can be used to study cannabis withdrawal.</p>

<p>Dimethandrolone Undecanoate (DMAU) is a novel orally available androgen with progestational activity and is a potential male contraceptive compound.</p>

<p>2-MNG (2-Mercaptonicotinoyl glycine) is a novel melanogenesis inhibitor. 2-MNG inhibits two mechanisms of UV-induced skin pigmentation in vivo.</p>