Dilmapimod (SB-681323) is a potent p38 MAPK inhibitor that potentially suppresses inflammation in chronic obstructive pulmonary disease. SB-681323 potently inhibits p38 MAPK signaling, measured by inhibition of sorbitol-induced pHSP27 expression. Dilmapimod (SB-681323) inhibited TNF-alpha production. The treatment with SB-681832 is a safe and effective means of reducing hsCRP in undergoing elective PCI.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||Soluble in DMSO|
A randomized, placebo-controlled study of the effects of the p38 MAPK inhibitor SB-681323 on blood biomarkers of inflammation in COPD patients.
Singh D, et al. J Clin Pharmacol. 2010 Jan;50(1):94-100. PMID: 19880675.
|Related p38 MAPK Products|
R1487 Hydrochloride is an orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.
Pamapimod is a novel p38 mitogen-activated protein kinase inhibitor, inhibited p38alpha and p38beta enzymatic activity, with IC50 values of 0.014 +/- 0.002 and 0.48 +/- 0.04 microM, respectively.
SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580.
SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po). IC50 value: 170 nM Target: p38MAPK
SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes.
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