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SB-505124

Cat. No. M2550
SB-505124 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 40  USD40 In stock
5mg USD 72  USD72 In stock
10mg USD 104  USD104 In stock
50mg USD 320  USD320 In stock
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Quality Control & Documentation
Biological Activity

SB-505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5), ALK4 and ALK7 (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively). SB-505124 also blocks more complex endpoints of TGF-beta action, as evidenced by its ability to abrogate cell death caused by TGF-beta1 treatment. SB-505124 is three to five times more potent than a related ALK5 inhibitor described previously, SB-431542.

Customer Product Validations & Biological Datas
Source Arthritis Res Ther (2017). Figure 1. SB-505124
Method Western Blot
Cell Lines Primary bovine chondrocytes
Concentrations 5 μM
Incubation Time 1 h
Results Subsequently, we analyzed the effects of the ALK4/5/7-kinase inhibitor SB-505124, the ALK1/2/3-kinase inhibitor LDN-193189 and the TAK1-kinase inhibitor (5Z)-7-Oxozeaenol on TGFβ1-induced R-Smad phosphorylation
Chemical Information
Molecular Weight 335.4
Formula C20H21N3O2
CAS Number 694433-59-5
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] DaCosta Byfield S, 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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