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

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

Art. -Nr.: HY-125856 Reinheit: 99.93%
COA
SDS
Handling Instructions 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 Chemische Struktur

CAS. Nr. : 1802425-99-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

Milvexian Related Antibodies

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Beschreibung

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].

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].

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

Milvexian Related Antibodies
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

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.
Klinische Studie
Molekulargewicht

626.44

Formel

C28H23Cl2F2N9O2
CAS. Nr.
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

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
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.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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
Reinheit & Dokumentation

Purity: 99.93%

SDS (252 KB)

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

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
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

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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