• 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。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *