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AMG131

Cat. No. M29897
AMG131 Structure
Synonym:

INT131

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Quality Control & Documentation
Biological Activity

AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM).

Chemical Information
Molecular Weight 514.21
Formula C21H12Cl4N2O3S
CAS Number 315224-26-1
Form Solid
Solubility (25°C) DMSO 250 mg/mL (ultrasonic)
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] Stergios A Polyzos, et al. Metabolism. Current and emerging pharmacological options for the treatment of nonalcoholic steatohepatitis

[2] Stergios A Polyzos, et al. Metabolism. Nonalcoholic fatty liver disease: Updates on associations with the metabolic syndrome and lipid profile and effects of treatment with PPAR-γ agonists

[3] Tongwei Yew, et al. Recent Pat Cardiovasc Drug Discov. Selective peroxisome proliferator-activated receptor-γ modulation to reduce cardiovascular risk in patients with insulin resistance

[4] Alykhan Motani, et al. J Mol Biol. INT131: a selective modulator of PPAR gamma

[5] Linda S Higgins, et al. PPAR Res. The Development of INT131 as a Selective PPARgamma Modulator: Approach to a Safer Insulin Sensitizer

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