gpcr

GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis.

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].

GPCR agonist-2 (4-(Cyclopropylamino)-3-nitrobenzoic acid) is an agonist of the orphan human GPCR GPR109B.

Azenosertib (ZN-c3) is an orally active, specific GPR119 agonist. Azenosertib (ZN-c3) stimulates cell proliferation and improves pancreatic β-cell function. [1]

MS48107 is a potent, selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68), demonstrating specificity for GPR68 over closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. It effectively crosses the blood-brain barrier (BBB) in mice.

Adenosine (D-Adenosine) is a natural product, a ribonucleoside consisting of adenine bound to ribose. Adenosine has vasodilatory, antiarrhythmic and analgesic effects.

Rasarfin inhibits Ras and ARF6.

7α,25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist, as well as an endogenous ligand, of the orphan GPCR receptor EBI2 (GPR183). It serves as a chemokine directing the migration of B cells, T cells, and dendritic cells and exhibits high potency in activating EBI2 (EC50=140 pM; Kd=450 pM) [1][2].

Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

Almorexant hydrochloride (ACT 078573 hydrochloride) is an orally active dual orexin receptor antagonist that blocks the intracellular Ca2+ signaling pathway and, to a certain extent, blocks the excitatory effects of methamphetamine. Almorexant hydrochloride Induces apoptosis and can be used to study sleep disorders.

Ro 5212773 (Epptb) is a selective TAAR1 antagonist.

Orphan GPCR SP9155 agonist P550 (mouse, rat) (26RFa (mouse, rat)) is an RFamide peptide family member with an orexigenic effect, acting as the cognate ligand for the mouse orphan receptor GPR103, also known as SP9155 or AQ27.

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.

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

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

CRTh2 antagonist 2 is a selective and potent CRTH2 antagonist, IC50≤10 nM. CRTh2 antagonist 2 can be used to study the direction of androgenic alopecia.

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.

GPR84 antagonist 8 is a selective GPR84 antagonist applicable for investigating inflammatory and fibrotic diseases.

Fezagepras sodium (Setogepram sodium salt) is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferative actions.

(1R,2R)-2-PCCA hydrochloride is a potent, selective, and blood-brain-barrier-crossing GPR88 receptor agonist with an EC50 value of 1140 n in striatal membranes of WT mice; it can be used to study the central nervous system.

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM, respectively.

YE 120 is a highly potent GPR35 agonist (EC50: 32.5 nM) with potential anti-inflammatory and anti-cancer activities, which can be used to study G protein-coupled receptor-related diseases.

FL104 is a potent agonist of small-molecule urotensin II receptor, pEC50= 7.11.