G-protein Coupled Receptors and 7-TM Receptors

ONO-9780307 is a specific antagonist of LPA1 (lysophosphatidic acid receptor 1) (IC50: 2.7 nM).

Compound 2o, also known as CB2R/5-HT1AR agonist 1, serves as a partial orally active agonist for the CB2 receptor (EC50 = 479.6 nM) and a full agonist for the 5-HT1A receptor (EC50 = 2.7 μM). This compound demonstrates both anti-anxiety and anti-depressive effects and has favorable pharmacokinetic properties [1].

Compound 1f, a potent MRGPRX1 agonist, has an EC50 of 0.22 μM, useful for neuropathic pain studies.

Monlunabant ((S)-MRI-1891), a solid dispersion compound, functions as an inhibitor of the cannabinoid CB1 receptor [1].

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

SSTR5 antagonist 6, an orally active antagonist specific to the somatostatin receptor subtype 5 (SSTR5), exhibits an IC50 value of 24 nM. This compound is utilized in researching type 2 diabetes [1].

IMP-1575 is a highly effective inhibitor of hedgehog acyltransferase (HHAT), with an IC50 of 0.75 μM when inhibiting purified HHAT. IMP-1575 has potential applications in cancer research.

5-HT1A antagonist; Ki=8nM, Kb=0.04nM. PDE4B IC50=80.4μM; PDE7A IC50=151.3μM. Good biofilm penetration, stable, anticognitive, antidepressant.

<p>AMG-369 (AMG 247) is an S1P1/S1P5 dual agonist that delays the development of experimental autoimmune encephalomyelitis in rats.</p>

<p>EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4, with an IC50 of 1.1 nM. This compound inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 of 0.9 nM. In RAW 264.7 macrophages, it reduces the expression of PGE2-induced IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C motif) ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase 1 (Arg1) mRNA. In the CT26 mouse colon cancer model, EP4 receptor antagonist 7, combined with an anti-PD-1 antibody, inhibits tumor growth and enhances CD8+ T cell infiltration into the tumor.</p>

RS 12254 is a dopamine agonist and antihypertensive agent.

NBI 35965 hydrochloride is a selective CRF1 (corticotropin-releasing factor receptor 1) antagonist that is both orally active and capable of penetrating the brain. It possesses a K i value of 4 nM and a pK i of 8.5, and does not affect CRF2. This compound effectively diminishes CRF or stress-triggered ACTH (adrenocorticotropic hormone) production in vivo, demonstrating pIC 50 values of 7.1 and 6.9. Additionally, NBI 35965 hydrochloride exhibits anxiolytic properties [1] [2].

P2Y2 and P2Y4 receptor agonist

<p>Compound (−)-19, also known as (-)-5-HT2C agonist-3, is a selective 5-HT2C agonist exhibiting a preference for Gq signaling. It demonstrates efficiency with EC50 values for 5-HT2 receptor subtypes as follows: 5-HT2C at 103 nM, 5-HT2B at 570 nM, and 5-HT2A at 72 nM. This compound is utilized in research on antipsychotics.</p>

GLP-1 Receptor Agonist 11 (compound 3) acts as an effective agonist for the GLP Receptor, finding use in research related to conditions like diabetes and non-alc. fatty liver disease [1].

<p>NCATS-SM4420 (Compound A35) is an orally effective ligand for the thyroid-stimulating hormone receptor (TSHR) that inhibits the proliferation of MDA-T32 and MDA-T85 cells both in vitro and in vivo, with IC50 values of 0.71 μM and 0.38 μM, respectively. Additionally, it suppresses the metastasis of MDA-T85F1 in mice. NCATS-SM4420 holds potential for research in the field of thyroid cancer.</p>

CP-608039 is a selective adenosine A3 receptor agonist for both human A3 and human A1 receptors.

MRGPRX2 modulator-1 (example 17), a modulator of the mas-related G-protein receptor X2 (MRGPRX2), is employed in studies focused on inflammation, pain, and autoimmune disorders [1].

Pareptide monohydrochloride is a metabolically stable analog of melatonin inhibitor (MIF).

GRPR antagonist-1 targets GRPR, kills specific cancer cells (e.g., PC3, Pan02, HGC-27), and promotes apoptosis by modulating Bcl-2 and Bax.

LAS195319 is a potent and selective inhaled PI3Kδ Inhibitor (IC50 = 0.5 nM) for the Treatment of Respiratory Diseases.

LAB687 (Compound 2a) is an inhibitor of microsomal triglyceride transfer protein (MTP) with an IC50 of 0.9 nM for inhibiting the secretion of apolipoprotein B (apoB) in HepG2 cells. Additionally, LAB687 acts as a Smoothened (Smo) antagonist, exhibiting IC50 values of 2.48 μM and 3.42 μM for mouse and human Smo receptors, respectively. This compound is effective in reducing triglyceride and low-density lipoprotein cholesterol (LDL-C) levels and in inhibiting the Hedgehog signaling pathway.

Quinagolide Free Base is a non-ergot dopamine D(2)-agonist.

AL 6598, a prodrug of PGD2 agonist AL 6556, reduces IOP by 53% at 1μg twice daily in monkeys; binds DP receptors with Ki of 3.2μM.

GLP-1 receptor agonist 15 (Example 4) is a GLP receptor agonist with an EC50 of 0.74 nM. It exhibits an IC50 of 10.1 μM against the hERG potassium ion channel. This compound is applicable for research in the diabetes field.

<p>Burapitant (SSR 240600) is a novel non-peptide tachykinin neurokinin 1 (NK) receptor antagonist with anti-coke oven and antidepressant activity.</p>

Thielavin B, from Thielavia terricola, inhibits prostaglandin E2 synthesis and reduces rat oedema.

OP-2507, a prostacyclin agonist, is used potentially for the treatment of hepatic insufficiency and hypertension.

PGD2 is involved in allergy, asthma, sleep, temperature regulation, inhibits clotting, and relaxes blood vessels; PGDM, its metabolite, is a biomarker.

Nolpitantium besilate is a neurokinin-1 receptor antagonist.

<p>Zaladenant is an adenosine receptor antagonist with antitumor properties.</p>

Potent 5-HT6/5-HT2A receptors dual antagonist with K i of 11 nM & 39 nM.

<p>S1PR1 agonist 1 is a potent agonist of S1PR1. S1PR1 agonist 1 has potential in autoimmune diseases.</p>

<p>F 14679 is a potent 5-HT1A agonist (pKi=10.23) with a maximum Ca2t response similar to 5-HT.</p>

<p>SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.</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>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 (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).

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

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

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

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

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

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

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

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).

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

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

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.

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

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

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.

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.

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.

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

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

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.

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

<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>

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).

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

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

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

<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>

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.

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

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

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

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

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>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>

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.

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

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.

<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>

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.

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

<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.

SB251023 is an agonist of β3-adrenoceptor.

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

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

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).

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.

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

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

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