AbMole| Losmapimod 洛批莫德(CAS号：585543-15-3)

Losmapimod (GW856553)一种是口服活性的p38 MAPK抑制剂，对p38α和p38β的pKi为8.1和7.6。Losmapimod通过抑制p38 MAP激酶而起作用，p38 MAP激酶在缺血状况引起的动脉粥样硬化和心力衰竭的发展中起着重要作用。Losmapimod（GW856553）通过减少PIC的产生减弱了人类的促炎症反应。

化学性质

分子量	383.46
分子式	C22H26FN3O2
CAS号	585543-15-3
溶解性（25°C）	DMSO 25 mg/mL Ethanol 30 mg/mL
储存条件	粉末型式       -20°C   3年；4°C   2年 溶于溶剂       -80°C   6个月；-20°C   1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.6078 mL	13.0392 mL	26.0783 mL
5 mM	0.5216 mL	2.6078 mL	5.2157 mL
10 mM	0.2608 mL	1.3039 mL	2.6078 mL

参考文献

[1] Waterworth DM, et al. J Am Heart Assoc. A low-frequency variant in MAPK14 provides mechanistic evidence of a link with myeloperoxidase: a prognostic cardiovascular risk marker.

[2] Newby LK, et al. Lancet. Losmapimod, a novel p38 mitogen-activated protein kinase inhibitor, in non-ST-segment elevation myocardial infarction: a randomised phase 2 trial.

[3] Inamdar A, et al. J Psychopharmacol. Evaluation of antidepressant properties of the p38 MAP kinase inhibitor losmapimod (GW856553) in Major Depressive Disorder: Results from two randomised, placebo-controlled, double-blind, multicentre studies using a Bayesian approach.

[4] Watz H, et al. Lancet Respir Med. Efficacy and safety of the p38 MAPK inhibitor losmapimod for patients with chronic obstructive pulmonary disease: a randomised, double-blind, placebo-controlled trial.

[5] Dewenter M, et al. Dtsch Med Wochenschr. Losmapimod: a novel drug against cardiovascular diseases?

[6] Barbour AM, et al. Br J Clin Pharmacol. Safety, tolerability, pharmacokinetics and pharmacodynamics of losmapimod following a single intravenous or oral dose in healthy volunteers.