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MedChemExpressModel Milvexian -1802425-99-5

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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].
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Milvexian

MCE China:Milvexian

Brand:MedChemExpress (MCE)

Cat. No.HY-125856

CAS:1802425-99-5

Synonyms:BMS-986177; JNJ-70033093

Purity:99.93%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description: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.

In Vitro: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].

In Vivo: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

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References:

[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).

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world;
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas;
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects;
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services;
•   It has a professional experimental center and strict quality control and verification system;
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•   The biological activity of the products has been verified by the experiments of customers in various countries;
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers;
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world;
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。