| 产品描述： | HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX |
| 靶点： |
IC50: 0.6 nM (HPGDS in enzyme assays) and 32 nM (HPGDS in cellular assays);PGESynthase |
| 体外研究： |
HPGDS inhibitor 1 has equal potency against purified HPGDS from human, rat, dog, and sheep (IC50, 0.5-2.3 nM) |
| 体内研究： |
HPGDS inhibitor 1 (compound 8; 1 mg/kg) has excellent PK characteristics with 76% bioavailability, and the T1/2 is 4.1 hours in rats. Rats dosed orally with 1 mg/kg and 10 mg/kg HPGDS inhibitor 1 (compound 8) are sacrificed at various times. Oral administration of HPGDS inhibitor 1 blocks PGD2 production in the rat spleen; inhibition of PGD2 is inversely correlated with the plasma concentration of HPGDS inhibitor 1 in a time- and dose-dependent manner. HPGDS inhibitor 1 (compound 8; 1 mg/mL) illustrates efficacy in an in vivo sheep model of asthma |
| 参考文献： |
1. Chris P Carron, et al. Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS). ACS Med Chem Lett. 2010 Feb 2;1(2):59-63. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.622 ml |
13.111 ml |
26.221 ml |
| 5 mM |
0.524 ml |
2.622 ml |
5.244 ml |
| 10 mM |
0.262 ml |
1.311 ml |
2.622 ml |
| 50 mM |
0.052 ml |
0.262 ml |
0.524 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京