Product Introduction
Bioactivity


英文名: HPGDS inhibitor 2

描述: HPGDS inhibitor 2 (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)。

体外活性: 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.

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 130mg/ml(343.54mM)


关键字: HPGDS inhibitor2 | PGE synthase | Inhibitor | inhibit | HPGDS inhibitor-2 | HPGDS inhibitor 2 | Prostaglandin E synthase

相关产品: Dehydroevodiamine | CAFESTOL | (S)-Flurbiprofen | Benzydamine hydrochloride | ETHYL CAFFEATE | Sinensetin | Friluglanstat | AT-56 | hPGDS-IN-1 | Limaprost

相关库: Bioactive Compounds Library Max | Inhibitor Library | NO PAINS Compound Library | Bioactive Compound Library