GPCR/G-Protein

TAAR1 agonist 2 (compound 30), a full agonist at trace amine-associated receptor 1 (TAAR1) (pEC50=7.5), also displays agonistic properties at H1 receptors and activates various muscarinic acetylcholine receptors, including the M2 receptor (pEC50=5). This compound is utilized in researching neuropsychiatric diseases.

Becondogrel (2-Oxoclopidogrel) is a metabolite of Clopidogrel. It irreversibly inhibits the P2Y12 receptor, thereby preventing platelet aggregation and thrombosis.

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.

Danavorexton is an orexin receptor agonist.

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.

SB-423557 is an orally active antagonist of calcium-sensing receptor (CaR) with IC50 of 520 nM

Pentacosafluorotridecanoic Acid (PFTrDA) is a perfluoroalkyl substance (PFAS) that exhibits various biological impacts across different species. In zebrafish embryos, exposure to PFTrDA induces yolk sac edema and increases mRNA expression of thyroid hormone synthesis genes, including tshβ, at concentrations of 0.1 and 0.3 mg/L. At a dosage of 10 mg/kg, PFTrDA reduces serum testosterone and luteinizing hormone levels, as well as palmitic acid, linoleic acid, and oleic acid levels in the testicular interstitial cells of late adolescent rats. In humans, maternal plasma levels of PFTrDA during pregnancy are positively correlated with the development of eczema in female infants (but not male infants), and PFTrDA levels are higher in the livers of cancerous humans compared to non-cancerous ones. Additionally, PFTrDA is found in marine mammals.

GLP-1 receptoragonist 16 (Example 53) is a GLP-1 agonist applicable for research in diabetes, obesity, or diseases related to non-alcoholic steatohepatitis.

RS 61756-007 is a selective thromboxane receptor (TP) agonist.

5-HT2/5-HT7 receptor antagonist

(R)-MrgprX2 antagonist-3 is an antagonist of MrgprX2. It is applicable in the study of inflammatory skin diseases. For more detailed information, please refer to compound E118 in patent document WO2021092240A1.

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.

DCB-3503, a tylophorine analog, may treat cancer and suppress immunity by blocking protein synthesis and modulating HSC70's ATPase activity.

Selective, high affinity competitive antagonist of the P2Y1 receptor

BI-685509: potent, oral sGC activator, boosts cGMP, enhances NO pathways, for CKD/DKD research.

M1069 is an oral A2A/A2B receptor antagonist, 100x more selective over A1/A3, with antitumor properties by blocking adenosine's immunosuppressive effects.

L-796778 acetate is a selective sst3 receptor agonist. In CHO-K1 cells expressing hsst3 receptors, it acts as a partial agonist that inhibits Forskolin-induced cAMP production, with an IC50 value of 18 nM. Additionally, L-796778 acetate exhibits anticonvulsant properties.

CVN766 is an orally active orexin 1 receptor antagonist with blood-brain permeability, demonstrating IC50 values of 8 nM for OX1R and >10 μM for OX2R. CVN766 can be used to study schizophrenia [1].

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,

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

<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>

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

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

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

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

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

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

AZD-5672 is an antagonist of CCR5 with an IC50 of 0.32 nM.

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

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

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

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

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

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.

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

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

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

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.

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

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.

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

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

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

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).

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.

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.

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.

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.

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.

(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.

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).

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.

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.

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).

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

<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>

N-methyl-2-AI (hydrochloride) is a useful organic compound for research related to life sciences. The catalog number is T66396 and the CAS number is 10408-85-2.

<p>Patecibart is a humanized immunoglobulin G4-kappa monoclonal antibody that functions as an antagonist to the endothelin receptor A (EDNRA).</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>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>Propiram fumarate HClis an orally available Opioid receptors agonist with analgesic activity for the study of musculoskeletal pain.</p>

SKF 89748 is an agonists of alpha 1-adrenoceptor.

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

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

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.

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

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

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

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

<p>Canagliflozin D4 is a deuterium-labeled Canagliflozin. Canagliflozin is an SGLT2 inhibitor.</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>RU 24969 succinate, a 5-HT receptor agonist, exhibits K i values of 0.38 nM for 5-HT 1B and 2.5 nM for 5-HT 1A, indicating its affinity towards these receptors. It reduces fluid consumption and enhances forward locomotion. This compound is utilized in neurological disease research.</p>

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

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.

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

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).

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

<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>

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

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