GSK-2894631A 是高效的造血前列腺素 D 合成酶(H-PGDS)选择性抑制剂(IC50:9.9 nM)。

HPGDS inhibitor 2 is a potent, selective hematopoietic prostaglandin D synthase (h-pgds) inhibitor, IC50 = 9.9 nm.

GSK2894631A(IC50 = 9.9 nM, LE = 0.42) is a potent, competitive, and reversible inhibitor of H-PGDS. GSK2894631A exhibited good H-PGDS cellular activity (RBL IC50 = 160 nM) in a rat basophilic leukemia (RBL) cell PGD2 production assay.

GSK2894631A had a low i.v. clearance (Cl = 5.6 mL/min/kg), moderate i.v. steady state volume of distribution (VSS = 1.7 l/kg), long i.v. terminal half-life (t1/2 = 3.8 hr), and good oral exposure (p.o. DNAUC = 1800 ng/hr/mL, F = 61%) in mice. It attenuated PGD2 production in an acute in vivo murine mast cell degranulation model (ED50 = 0.032 mg/kg, EC50 = 21 nM) of inflammation. Unfortunately, at higher doses (≥10 mg/kg) in a chronic eccentric muscle damage model (vide infra Fig. 6) in mice, 1a-treated animals exhibited seizure-like activity at day four of dosing.

2101626-26-8

C20H24F2N2O3

378.42

GSK-2894631A

DMSO:130mg/ml(343.54mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years