产品说明书

Dilmapimod

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Chemical Structure| 444606-18-2 同义名 : Sb-681323;GW 681323
CAS号 : 444606-18-2
货号 : A724338
分子式 : C23H19F3N4O3
纯度 : 99%+
分子量 : 456.417
MDL号 : MFCD16659063
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(262.92 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The p38 mitogen-activated protein kinase (MAPK) signaling upregulates inflammation and is known to be increased in chronic obstructive pulmonary disease (COPD). Dilmapimod is a specific inhibitor of p38 MAPKα, with approximately 15-fold selectivity over the closest structurally related p38 isoform, p38β-2, and more than 5000-fold selectivity over p38γ and p38δ. Treatment with dilmapimod significantly reduced pHSP27 levels up to 6 hours postdose compared with placebo, demonstrating in vivo inhibition of p38 MAPK. Furthermore, the maximal inhibition of LPS (lipopolysaccharide)-induced TNF-α (tumor necrosis factor) production was observed at 1 hour postdose for both doses of dilmapimod (7.5 and 25 mg). For dilmapimod (25 mg), significant inhibition was sustained up to 6 hours[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.95mL

2.19mL

1.10mL

21.91mL

4.38mL

2.19mL
参考文献

[1]Singh D, Smyth L, Borrill Z, Sweeney L, Tal-Singer R. A randomized, placebo-controlled study of the effects of the p38 MAPK inhibitor SB-681323 on blood biomarkers of inflammation in COPD patients. J Clin Pharmacol. 2010;50(1):94-100