2. Metabolic Enzyme/Protease
  3. Factor Xa
  4. Milvexian

Milvexian  (Synonyms: BMS-986177; JNJ-70033093)

製品番号: HY-125856 純度: 99.93%
COA 取扱説明書 Technical Support

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.

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Milvexian

Milvexian 構造式

CAS 番号 : 1802425-99-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1654 在庫あり
Solution
10 mM * 1 mL in DMSO USD 1654 在庫あり
Solid
1 mg $600 在庫あり
5 mg $1200 在庫あり
10 mg $1800 在庫あり
25 mg $3240 在庫あり
50 mg $4536 在庫あり
100 mg $6350 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 2 publication(s) in Google Scholar

Milvexian 関連抗体

Top Publications Citing Use of Products

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

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].

体外実験

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 関連抗体
体内実験

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: The rabbit electrically mediated carotid arterial thrombosis model[1]
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
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.
Animal Model: The rabbit cuticle bleeding time model[1]
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
Result: Did not increase the carotid blood flow(BT) with combination of Aspirin (HY-14654).
Animal Model: The rabbit arteriovenous shunt model[2]
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
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.
臨床実験
分子量

626.44

分子式

C28H23Cl2F2N9O2
CAS 番号
Appearance

Solid

Color

White to off-white

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5963 mL 7.9816 mL 15.9632 mL
5 mM 0.3193 mL 1.5963 mL 3.1926 mL
10 mM 0.1596 mL 0.7982 mL 1.5963 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション

純度: 99.93%

COA (255 KB) HNMR (287 KB) LCMS (91 KB)

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
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Milvexian Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Milvexian1802425-99-5BMS-986177 JNJ-70033093BMS986177BMS 986177JNJ70033093JNJ 70033093JNJ-70033093Factor XaFxaantithromboticblood coagulationfactor XIa inhibitorhemostasisthe ECAT modelthe cuticle BT modelthe AV shunt modelInhibitorinhibitorinhibit

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