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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.93%
- CAS 番号: 1802425-99-5
- 分子式: C28H23Cl2F2N9O2
- 分子量:626.44
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Milvexian
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生物活性
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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1802425-99-5
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性状 Solid
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分子量 626.44
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分子式 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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別名
BMS-986177; JNJ-70033093
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (282 KB)
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SDS (252 KB)
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- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 |
|---|---|---|---|---|---|
| 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 関連分類
HY-125856 関連分類
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