Milvexian
Based on 2 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.93%
- CAS. Nr.: 1802425-99-5
- Formel: C28H23Cl2F2N9O2
- Molecular Weight:626.44
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Milvexian
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Biologische Aktivität
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The rabbit electrically mediated carotid arterial thrombosis model[1]
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Dosage:Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)
Treatment: 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h) -
Administration:Intravenous injection (i.v.) plus a continuous infusion
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Result:Decreased carotid blood flow(CBF) to 32-76% and reduced thrombus weight by 15-70%.
Decreased CBF to 40% of control initiated after 15 min.
Decreased CBF to 39-66% after Seventy-five minutes.
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Animal Model:The rabbit cuticle bleeding time model[1]
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Dosage:Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)
Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)
Treatment: 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h) -
Administration:Intravenous injection (i.v.) plus a continuous infusion
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Result:Did not increase the carotid blood flow(BT) with combination of Aspirin (HY-14654).
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Animal Model:The rabbit arteriovenous shunt model[2]
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Dosage:Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)
Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h) 0.25 + 0.17, 1.0 + 0.67, and 4.0 + 2.68 mg/kg -
Administration:Intravenous injection (i.v.) plus a continuous infusion
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Result:Reduced thrombus weight of thrombosis by 34.3 -66.9 %.
Increased the prolongation of APTT with 1.54-3.12-fold, but did not alter the PT and TT.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1802425-99-5
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Appearance Solid
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Molecular Weight 626.44
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Formel C28H23Cl2F2N9O2
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Color White to off-white
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SMILES
O=C(NC1=C2N(C(F)F)N=C1)[C@H](C)CCC[C@H](N(C=NC(C3=CC(Cl)=CC=C3N4N=NC(Cl)=C4)=C5)C5=O)C6=CC2=CC=N6
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Synonyms
BMS-986177; JNJ-70033093
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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J Thromb Haemost
Interferences associated with the factor XIa inhibitors asundexian and milvexian in routine and specialized coagulation assays and their removal by activated charcoal-based adsorbents. [Abstract]2025 Jun 9:S1538-7836(25)00354-X. PMID: 40499719 -
Diagnostics (Basel)
Laboratory Evaluation of Interferences Associated with Factor XIa Inhibitors Asundexian and Milvexian in Routine Coagulation Assays. [Abstract]2024 Sep 9;14(17):1991. PMID: 39272775
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (159.63 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.5963 mL | 7.9816 mL | 15.9632 mL | 39.9081 mL |
| 5 mM | 0.3193 mL | 1.5963 mL | 3.1926 mL | 7.9816 mL | |
| 10 mM | 0.1596 mL | 0.7982 mL | 1.5963 mL | 3.9908 mL | |
| 15 mM | 0.1064 mL | 0.5321 mL | 1.0642 mL | 2.6605 mL | |
| 20 mM | 0.0798 mL | 0.3991 mL | 0.7982 mL | 1.9954 mL | |
| 25 mM | 0.0639 mL | 0.3193 mL | 0.6385 mL | 1.5963 mL | |
| 30 mM | 0.0532 mL | 0.2661 mL | 0.5321 mL | 1.3303 mL | |
| 40 mM | 0.0399 mL | 0.1995 mL | 0.3991 mL | 0.9977 mL | |
| 50 mM | 0.0319 mL | 0.1596 mL | 0.3193 mL | 0.7982 mL | |
| 60 mM | 0.0266 mL | 0.1330 mL | 0.2661 mL | 0.6651 mL | |
| 80 mM | 0.0200 mL | 0.0998 mL | 0.1995 mL | 0.4989 mL | |
| 100 mM | 0.0160 mL | 0.0798 mL | 0.1596 mL | 0.3991 mL |
Milvexian Related Classifications
HY-125856 Related Classifications
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