For research use only. Not for therapeutic Use.
Milvexian is an orally bioavailable, small-molecule, reversible, direct antagonists of factor Xia, with the Ki of 0.11, 0.38, 0.64, 490, 350 nM for human, rabbit, dog, rat, mouse, respectively. Milvexian shows anti-thrombosis activity in vitro and in vivo, and can be used for thrombus study[1].
Milvexian (10 μM, approximately) increases activated partial thromboplastin time (APTT) in human plasma, but does not alter platelet aggregation responsed to ADP, arachidonic acid, and collagen in human plasma[1].
Milvexian (20 mg/kg for PO) produces average plasma concentrations of 2000 and 40 nM at 1 and 24 h after dosing, respectively[1].
Milvexian (0.8 mg/kg for i.v.) produces average plasma concentrations of 2000 and 100 nM at 10 min and 8 h after dosing, respectively[1].
Milvexian (0.063-4 + 0.04- 2.68 mg/kg for i.v. plus a continuous infusion) inhibites the formation of thrombosis in vivo[2].
Pharmacokinetic Analysis in Rabbits[1]
Route
Dose (mg/kg)
Clearance (mL/min/kg)
Volume of Distribution (L/kgL)
Half-life (h)
Oral Bioavailability (%)
i.v./p.o.
0.8/20
6.7
1.4
2.5
14
| Catalog Number | I032295 |
| CAS Number | 1802425-99-5 |
| Synonyms | (9R,13S)-13-[4-[5-chloro-2-(4-chlorotriazol-1-yl)phenyl]-6-oxopyrimidin-1-yl]-3-(difluoromethyl)-9-methyl-3,4,7,15-tetrazatricyclo[12.3.1.02,6]octadeca-1(18),2(6),4,14,16-pentaen-8-one |
| Molecular Formula | C28H23Cl2F2N9O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C28H23Cl2F2N9O2/c1-15-3-2-4-23(20-9-16(7-8-33-20)26-21(36-27(15)43)12-35-41(26)28(31)32)39-14-34-19(11-25(39)42)18-10-17(29)5-6-22(18)40-13-24(30)37-38-40/h5-15,23,28H,2-4H2,1H3,(H,36,43)/t15-,23+/m1/s1 |
| InChIKey | FSWFYCYPTDLKON-CMJOXMDJSA-N |
| SMILES | CC1CCCC(C2=NC=CC(=C2)C3=C(C=NN3C(F)F)NC1=O)N4C=NC(=CC4=O)C5=C(C=CC(=C5)Cl)N6C=C(N=N6)Cl |
| Reference | [1]. Pancras C. Wong, et al. Milvexian, an orally bioavailable, small‐molecule, reversible, direct inhibitor of factor XIa: In vitro studies and in vivo evaluation in experimental thrombosis in rabbits. [2]. Xinkang Wang, et al. Antithrombotic Effects of the Novel Small-Molecule Factor XIa Inhibitor Milvexian in a Rabbit Arteriovenous Shunt Model of Venous Thrombosis. TH Open. 2023 Apr; 7(2): e97–e104. [3]. Wong P, et al. Small-Molecule Factor XIa Inhibitor, BMS-986177/JNJ-70033093, Prevents and Treats Arterial Thrombosis in Rabbits at Doses that Preserve Hemostasis [abstract]. Res Pract Thromb Haemost. 2020; 4 (Suppl 1). |
