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货号:A724338 同义名: Sb-681323;GW 681323

Dilmapimod is a selective p38 MAPK inhibitor. It is used in neuropathic pain and acute respiratory distress syndrome.

Dilmapimod 化学结构 CAS号:444606-18-2
Dilmapimod 化学结构
CAS号:444606-18-2
Dilmapimod 3D分子结构
CAS号:444606-18-2
Dilmapimod 化学结构 CAS号:444606-18-2
Dilmapimod 3D分子结构 CAS号:444606-18-2
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Dilmapimod 纯度/质量文件 产品仅供科研

货号:A724338 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 p38 MAPK p38α p38β 其他靶点 纯度
BMS-582949 +++

p38 MAPK, IC50: 13 nM

98%
SB 203580 99%+
Pexmetinib Tie-2 99%+
Skepinone-L ++++

p38α, IC50: 5 nM

98%
Doramapimod ++++

p38α, Kd: 0.1 nM

p38α, IC50: 38 nM

99%+
VX-702 99%+
Ralimetinib dimesylate ++++

p38α, IC50: 7 nM

98%
SB 202190 ++

p38α, IC50: 50 nM

++

p38β, IC50: 100 nM

99%+
Losmapimod ++++

p38α, pKi: 8.1

+++

p38β, pKi: 7.6

99%+
Neflamapimod +++

p38α, IC50: 10 nM

+

p38β, IC50: 220 nM

99%+
PH-797804 ++

p38α, IC50: 26 nM

+

p38β, IC50: 102 nM

98%
TAK-715 ++++

p38α, IC50: 7.1 nM

+

p38β, IC50: 0.20 μM

99%+
SB 239063 ++

p38α, IC50: 44 nM

++

p38β, IC50: 44 nM

99%+
Pamapimod +++

p38α, IC50: 0.014 μM

+

p38β, IC50: 0.48 μM

98%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Dilmapimod 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].

Dilmapimod 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

Dilmapimod 实验方案

计算器
存储液制备 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

Dilmapimod 技术信息

CAS号444606-18-2
分子式C23H19F3N4O3
分子量 456.417
别名 Sb-681323;GW 681323
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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