GW788388 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5) (IC50 values are 0.018 and 0.093 μM for ALK5 binding and for TGF-β cellular assay respectively). GW788388 inhibits esophageal squamous cell carcinoma (ESCC)-induced neoangiogenesis. GW788388 is orally available with a half-life of approximately 4 hours. GW788388 blocked TGF-beta-induced Smad activation and target gene expression, while decreasing epithelial-mesenchymal transitions and fibrogenesis. Treatment with GW788388 significantly reduced TGF-beta activity, leading to the attenuation of systolic dysfunction and left ventricular remodeling in an experimental rat model of MI.
|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||DMSO 20 mg/mL|
Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction.
Tan SM, et al. Am J Physiol Heart Circ Physiol. 2010 May;298(5):H1415-25. PMID: 20154262.
Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis.
Petersen M, et al. Kidney Int. 2008 Mar;73(6):705-15. PMID: 18075500.
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LY3200882 is a novel, highly selective TGFβRI small molecule inhibitor.
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