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GW788388

Cat. No. M2000
GW788388 Structure
Size Price Availability Quantity
10mg USD 100 In stock
50mg USD 320 In stock
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Quality Control
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 425.48
Formula C25H23N5O2
CAS Number 452342-67-5
Purity 99.50%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GW788388 supplier, TGF-beta, inhibitors

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