货号	规格	价格	上海	北京	武汉	南京
S87961-1mg	≥98%	￥1000.00 S87961-1mg ￥1000.00 现货	10 10	-	-	-
S87961-5mg	≥98%	￥2500.00 S87961-5mg ￥2500.00 现货	10 10	-	-	-
S87961-10mg	≥98%	￥4000.00 S87961-10mg ￥4000.00 现货	8 8	-	-	-
S87961-25mg	≥98%	￥7812.00 S87961-25mg ￥7812.00 现货	5 5	-	-	-
S87961-50mg	≥98%	￥12500.00 S87961-50mg ￥12500.00 现货	3 3	-	-	-
S87961-100mg	≥98%	￥20000.00 S87961-100mg ￥20000.00 现货	2 2	-	-	-

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产品介绍

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

靶点：

PGE Synthase;PGESynthase

体外研究：

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

体内研究：

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.

参考文献：

1. Rc A , Dnd A , Yd A , et al. The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure[J]. Bioorganic & Medicinal Chemistry, 2020, 28( 23).

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.643 ml	13.213 ml	26.426 ml
5 mM	0.529 ml	2.643 ml	5.285 ml
10 mM	0.264 ml	1.321 ml	2.643 ml
50 mM	0.053 ml	0.264 ml	0.529 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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