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SAR441566

Cat. No. M31423
SAR441566 Structure
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Biological Activity

SAR441566 is an orally active TNF-α inhibitor that blocks the interaction of TNFα with TNFR1 by distorting the conformation of the soluble TNFα trimer and does not affect signaling of TNFα bound to cell membranes, and can be used in rheumatoid arthritis-related studies.

Chemical Information
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] Alexander Vugler, et al. Front Pharmacol. An orally available small molecule that targets soluble TNF to deliver anti-TNF biologic-like efficacy in rheumatoid arthritis

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Keywords: SAR441566 supplier, TNF Receptor, inhibitors, activators


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