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SB-505124 hydrochloride 

Cat. No. M29975
SB-505124 hydrochloride  Structure
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Quality Control & Documentation
Biological Activity

SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

Chemical Information
Molecular Weight 371.86
Formula C20H22ClN3O2
CAS Number 356559-13-2
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Joyce Aarts, et al. Sci Rep. Local inhibition of TGF-β1 signaling improves Th17/Treg balance but not joint pathology during experimental arthritis

[2] Jiayu Jiang, et al. J Pharm Biomed Anal. Development and validation of an LC-MS/MS method for the determination of SB-505124 in rat plasma: Application to pharmacokinetic study

[3] Vijaykumar Sutariya, et al. Pharm Dev Technol. Thermoreversible gel for delivery of activin receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery

[4] Jennifer Sapitro, et al. Mol Vis. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor

[5] Stacey DaCosta Byfield, et al. Mol Pharmacol. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7

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  Catalog
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Keywords: SB-505124 hydrochloride  supplier, TGF-β Receptor, inhibitors, activators


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