MRS2690

MRS2690 is a selective P2Y14 receptor agonist. MRS2690 inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 induces intracellular calcium mobilization, activates P38 and stimulates [³⁵S]GTPγS binding to RBL-2H3 cell membranes. MRS2690 enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release. MRS2690can be used for ischemic heart disease^[1][2][3][4]. In Vitro:MRS2690 (0.001-10 μM) elicits concentration-dependent contractions of porcine isolated coronary arteries at basal tone (log EC₅₀ = 6.30 M)^[1].
MRS2690 (0.001-10 μM) shows enhanced concentration-dependent contractile responses in porcine coronary arteries pre-treated with Forskolin (HY-15371) plus U46619 (HY-108566) (R_max = 1.77 g),which can be blocked by the P2Y14 antagonist PPTN (HY-110322A), but not affected by the P2Y6 antagonist MRS2578 (HY-13104)^[1].
MRS2690 (10 μM) significantly reduces forskolin-induced VASP phosphorylation (an indicator of cAMP levels) in porcine coronary arteries^[1].
MRS2690 (0.0001-1000 nM) induces intracellular calcium mobilization in RBL-2H3 cells in a concentration-dependent manner with an EC₅₀ of 538 nM^[2].
MRS2690 (0.0001-100 nM) stimulates [³⁵S]GTPγS binding to RBL-2H3 cell membranes in a concentration-dependent manner with an EC₅₀ of 8.1 nM^[2].
MRS2690 (1 μM) activates P38 mitogen-activated protein kinase (MAPK) in RBL-2H3 cells^[2].
MRS2690 alone cannot induce β-hexosaminidase (HEX) release, but it concentration-dependently enhances antigen (DNP-BSA)-induced HEX release in RBL-2H3 cells primed with anti-DNP-BSA antibody, with an EC₅₀ of 103 nM^[2].
MRS2690 (1 μM, 50 min) significantly enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release in LAD2 cells^[3].
MRS2690 (10-1000 nM) significantly induces platelet-dependent neutrophil chemotaxis towards Macrophage derived chemokine (MDC, CCL22) in a concentration-dependent manner^[4].