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BMS-986202

Cat. No. M21298
BMS-986202  Structure
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Biological Activity

BMS-986202 is a potent, selective, orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 of 14 μM. BMS-986202 can be used in IL-23-driven echinococcosis BMS-986202 can be used in studies of IL-23-driven echinococcosis, anti-CD40-induced colitis and spontaneous lupus.

Chemical Information
Molecular Weight 439.46
Formula C22H18D3FN6O3
CAS Number 1771691-34-9
Solubility (25°C) DMSO ≥ 200 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] Chunjian Liu, et al. J Med Chem. Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2

[2] Jonathan Ellery, et al. Eur J Pharmacol. Identification of compounds acting as negative allosteric modulators of the LPA1 receptor

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  Catalog
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