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R-268712

Cat. No. M9223
R-268712 Structure
Size Price Availability
5mg USD 175 1-2 Weeks
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). Oral administration of R-268712 at doses of 1, 3 and 10mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. R-268712 reduced proteinuria and glomerulosclerosis significantly with improvement of renal function. R-268712 could suppress glomerulonephritis as well as glomerulosclerosis by an inhibitory mechanism that involves suppression of TGF-β signaling.

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 363.39
Formula C20H18FN5O
CAS Number 879487-87-3
Purity >98%
Solubility DMSO: ≥ 90 mg/mL
Storage at -20°C
References

R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model.
Terashima H, et al. Eur J Pharmacol. 2014 Jul 5;734:60-6. PMID: 24726873.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: R-268712 supplier, TGF-beta/Smad, inhibitors

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