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Milvexian

Cat. No. M21191
Milvexian Structure
Synonym:

BMS-986177; JNJ-70033093

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Biological Activity

Milvexian (BMS-986177) is an orally bioavailable, reversible, direct inhibitor of human and rabbit factor (FXIa) with Ki values of 0.11 nM and 0.38 nM, respectively.

Chemical Information
Molecular Weight 626.44
Formula C28H23Cl2F2N9O2
CAS Number 1802425-99-5
Solubility (25°C) N/A
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] Vidya Perera, et al. Sci Rep. Safety, pharmacokinetics, and pharmacodynamics of milvexian in healthy Japanese participants

[2] Vidya Perera, et al. Clin Pharmacokinet. Single-Dose Pharmacokinetics of Milvexian in Participants with Mild or Moderate Hepatic Impairment Compared with Healthy Participants

[3] Jeffrey I Weitz, et al. N Engl J Med. Milvexian for the Prevention of Venous Thromboembolism

[4] Pancras C Wong, et al. J Thromb Haemost. Milvexian, an orally bioavailable, small-molecule, reversible, direct inhibitor of factor XIa: In vitro studies and in vivo evaluation in experimental thrombosis in rabbits

[5] Vidya Perera, et al. Clin Transl Sci. First-in-human study of milvexian, an oral, direct, small molecule factor XIa inhibitor

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Keywords: Milvexian, BMS-986177; JNJ-70033093 supplier, Factor Xa, inhibitors, activators

 
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