G-protein Coupled Receptors and 7-TM Receptors

<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>

(Rac)-BI 703704 is a potent activator of soluble guanylyl cyclase (sGC).

GLP-1R modulator-1 (Compound 384) is a potent and orally active selective agonist of the glucagon-like peptide-1 receptor (GLP-1R). It activates G protein-coupled signaling, leading to increased intracellular cAMP levels, enhanced insulin secretion, delayed gastric emptying, and reduced appetite. GLP-1R modulator-1 holds potential for research in type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

Lisuride: an oral D2 dopamine agonist, ergot derivative, used in Parkinson's, migraine, and high prolactin research.

Diosuxentan is an inhibitor of ETA and is utilized in research pertaining to cardiovascular, renal, and neuronal inflammatory 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.

RXFP1 receptor agonist-10 (Compound 188) is an RXFP1 receptor agonist with an EC50 of 0.5 nM. It is useful for research into heart failure.

RGS10 modulator-1 (compound 15) is an effective regulator of RGS10. It significantly reverses IFNγ-induced expression of both RGS10 protein and mRNA, as well as COX-2 mRNA and iNOS expression triggered by IFNγ.

AM11638 is an endogenous cannabinoid analogue that targets cannabinoid receptors (CB1 and CB2 receptors), exhibiting analgesic properties. It shows potential for research in neurological disorders and inflammation-related diseases.

<p>Gemilukast (ONO-6950) is a cysteinyl leukotriene 1 and 2 receptor inhibitor that inhibits bronchoconstriction and is used in the treatment of asthma.</p>

Tonapofylline, orally active, selectively blocks A1 adenosine receptor (Ki: 7.4 nM), used in heart failure research.

LPA5 antagonist 2, compound 65, water-soluble, reduces nociception, for inflammatory/neuropathic pain study.

ZD6021 is an antagonist of neurokinin 1 receptor.

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

Potent CB1/2 agonist 1; crosses blood-brain barrier; anti-inflammatory, analgesic; for multiple sclerosis research.

CCR7-Cmp2105 is a thiadiazole-dioxide allosteric antagonist for CCR7 with a Kd of 3 nM and IC50 of 7.3 μM against arrestin binding.

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

Nocloprost (SH 475) is a prostaglandin E2 (PGE2) analog, an EP1 and EP3 receptor agonist with local gastric protection and ulcer healing effects.

GAT564, an allosteric CB1R modulator, shows EC50s of 87 nM (cAMP) & 320 nM (β-arrestin2) and lowers IOP effectively in glaucoma mice.

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

Ro 24-4736 is an effective and selective platelet-activating factor antagonist.

Rocavorexant is an antagonist of the orexin-1 receptor (orexin-1 receptor), exhibiting a pIC50 value of 9.1 for human OX1 and a pIC50 of 6.0 for human OX2.

CCR3 antagonist2 (example 66) is a CCR3 antagonist useful for researching inflammatory or allergic diseases, particularly those affecting the respiratory tract, such as inflammatory or obstructive airway conditions.

KARI 201 hydrochloride is a selective, brain-penetrant, competitive inhibitor of acid sphingomyelinase (ASM) with an IC50 of 338.3 nM. It also acts as an agonist for the growth hormone-releasing peptide receptor (ghrelin receptor). Additionally, KARI 201 hydrochloride can enhance the neuropathological features of Alzheimer's disease.

CP-199330: non-toxic alternative to Zafirlukast & Pranlukast, blocks cysteyl LT1 receptors.

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

Cendifensine functions as a monoamine reuptake inhibitor, targeting the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT).

Iloprost, a potent prostacyclin analog, binds to human IP & EP1 receptors with high affinity; inhibits platelet aggregation effectively.

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

BMS-986120: Oral, reversible PAR4 antagonist. IC50: 9.5 nM (human), 2.1 nM (monkey). Potent, selective antiplatelet.

VU0514009 is a competitive antagonist of chemokine-like receptor 1 (CMKLR1) with an EC50 of 2 nM. It effectively inhibits chemerin-9-induced arrestin recruitment and receptor internalization, significantly reducing Ca2+ flux responses in HEK293 cells. This compound shows potential for research in inflammatory diseases and metabolic syndrome.

NPR-C activator 1 is an activator of the natriuretic peptide receptor C (NPR-C), which can be used to study cardiovascular diseases.

Compound 23: H3R antagonist with 170 nM Ki; inhibits AChE, BChE, hMAO B; IC50s: 180, 880, 775 nM; anti-pain, memory boost; crosses BBB. [1]

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

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

<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>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>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>

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

<p>PF-07258669 is a selective melanocortin 4 receptor (MC4) antagonist used in the study of cachexia and loss of appetite.</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>Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist.Cost-effective and quality-assured.</p>

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

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

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

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

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.

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.

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

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

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.

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

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.

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

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

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

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

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).

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

<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>

SKF 89748 is an agonists of alpha 1-adrenoceptor.

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

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>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>

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.

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

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

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

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

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

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.

<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.

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.

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

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

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>

<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.