S81772 |
HPGDS inhibitor 1 |
源叶(MedMol) | 99% |
- 提示:详情请下载说明书。
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)