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HPGDS inhibitor 2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HPGDS inhibitor 2图片
CAS NO:2101626-26-8
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
GSK-2894631A
产品介绍
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)。

产品描述

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

Cas No.

2101626-26-8

分子式

C20H24F2N2O3

分子量

378.42

别名

GSK-2894631A

储存和溶解度

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