GPCR

Fulvestrant-d3 is a isotope labeled compound of Fulvestrant.Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist and GPR30 agonist that inhibits cell proliferation and induces apoptosis and autophagy.

NOX-6-18 (GPR132-B-160) is a highly potent and selective GPR132 antagonist with insulinotropic activity that modulates macrophage reprogramming in pancreatic islets and reduces weight gain.

BTB09089 (GPR65 agonist ) is a T cell death-associated gene 8 (TDAG8 GPR65)-specific agonist.BTB09089 induces TDAG8 expression and regulates cytokine production in T cells and macrophages.

GLPG0974 is an antagonist of FFA2 GPR43 with IC50 of 9 nM.

CAY10595 is an antagonist of the CRTh2 (DP2) receptor with a Ki of 10 nM.

TAK-041 (NBI-1065846) is a potent and selective GPR139 agonist.

GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK PD characteristics and can be used to study pulmonary fibrosis.

G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM).

Fasiglifam (TAK875) is a potent, selective and orally bioavailable GPR40 agonist.

ONC212 [a fluorinated-ONC201 analogue] is a selective GPR132 agonist.

Prosaptide TX14(A) acetate is a potent GPR37L1 and GPR37 agonist. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells.

VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.

Cangrelor tetrasodium is a reversible and selective antagonist of platelet P2Y12, with prompt and potent antiplatelet effects.

LY2881835 is a potent and selective GPR40 agonist.

CID 2745687 is a moderately potent, concentration-dependent antagonist at human GPR35 with pIC50 = 6.70. CID 2745687 cannot effectively antagonize the agonist effects of either Zaprinast or Cromolyn disodium at rodent ortholog of GPR35 in vitro[1]. However, CID 2745687 can reverse lodoxamide-mediated anti-fibrotic effects in mice in vivo[2].

CRTh2 antagonist 1 is a CRTh2 antagonist [IC50: 89 nM].

AM251 is a effective CB1 receptor antagonist (IC50 Ki: 8 7.49 nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 nM).

BIM-46174 HCl is a selective G protein inhibitor with anticancer activity that inhibits the growth of a large number of human cancer cell lines and induces cysteine 3-dependent apoptosis.

HA15 targets specifically BiP GRP78 HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.

MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM).

Bimatoprost acid (17-phenyl trinor PGF2α) is a metabolically stable analog of PGF2α and has a potential antagonistic activity for the FP receptor. It has a relative potency of 756% compared to PGF2α for binding to the FP receptor on ovine luteal cells.

LY2922470 reduces glucose levels along with significant enhancements in insulin and GLP-1, which is the potential for the treatment of type 2 diabetes mellitus (T2DM). LY2922470 is an effective, selective, and orally available agonist of the G protein-cou

Latanoprost (Xalatan) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.

hGPR91 antagonist 3 is an orally active, potent, and selective hGPR91 antagonist. hGPR91 antagonist 3 is used to study hypertension, autoimmune diseases, and retinal angiogenesis. hGPR91 antagonist 3 has been shown to be effective in the treatment of hypertension, autoimmune disease, and retinal angiogenesis.