In vitro: SKF-86002 inhibited prostaglandin H2 (PGH2) synthase activity (IC50 120 microM) as well as prostanoid production by rat basophilic leukemia (RBL-1) cells (IC50 70 microM) and its sonicate (IC50 100 microM) and human monocytes (IC50 1 microM). In addition, SK&F 86002 inhibited the generation of dihydroxyeicosatetraenoic acid (diHETE) and 5-hydroxyeicosatetraenoic acid (5-HETE) by a high speed supernatant fraction of RBL-1 cells (IC50 10 microM). differentiation of HL-60 cells toward the neutrophil phenotype resulted in a loss in c-Jun NH2-terminal kinase activation with concomitant acquisition of formylmethionylleucylphenylalanine-stimulatable and stress-inducible p38 MAPK activity as well as apoptosis blockade by SKF-86002. SKF-86002 blocked superoxide anion production in response to FMLP and reduced adhesion and chemotaxis in response to PAF or FMLP.
|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||10 mM in DMSO|
p38 MAPK Inhibition Improves Synaptic Plasticity and Memory in Angiotensin II-dependent Hypertensive Mice.
Dai HL, et al. Sci Rep. 2016 Jun 10;6:27600. PMID: 27283322.
Suppression of problematic compound oligomerization by cosolubilization of nondetergent sulfobetaines.
Mizukoshi Y, et al. ChemMedChem. 2015 Apr;10(4):736-41. PMID: 25760302.
|Related p38 MAPK Products|
GS-444217 is a potent and selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87±0.85 nM.
BMS-582949 is a potent and selective P38 mitogen-activated protein kinase (P38 MAPK) inhibitor with IC50 of 13nM.
R1487 Hydrochloride is an orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.
Dilmapimod (also known as SB-681323 and GW-681323) is a p38 MAPK inhibitor that potentially suppresses inflammation in COPD.
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.
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