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.
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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。 |
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]. |
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 |
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 |