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

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

目录号: HY-125856 纯度: 99.36%
COA 产品使用指南

Milvexian 是一种口服有效、小分子、可逆、直接结合的 factor Xia 拮抗剂,对人、兔、狗、大鼠和小鼠的 Ki 值分别为 0.11、0.38、0.64、490、350 nM。Milvexian 在体内外表现出抗血栓活性,可用于血栓研究。

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Milvexian Chemical Structure

Milvexian Chemical Structure

CAS No. : 1802425-99-5

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1 mg ¥6000
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

Milvexian (约10 μM) 可增加人血浆中活化部分凝血活素时间,对人血浆中 ADP 、花生四烯酸和胶原蛋白对血小板聚集没有影响[1]

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

体内研究
(In Vivo)

Milvexian (20 mg/kg, 口服) 给药后 1 和 24 小时的平均血浆浓度分别为 2000 和 40 nM[1]
Milvexian (0.8 mg/kg, 静脉注射) 给药后 10 分钟 和 8 小时的平均血浆浓度分别为 2000 和 100 nM[1]
Milvexian (0.063-4 + 0.04- 2.68 mg/kg, 静脉滴注加持续输注) 可以抑制体内血栓形成[2]

在兔中的药代动力学分析[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

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.
Clinical Trial
分子量

626.44

Formula

C28H23Cl2F2N9O2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 100 mg/mL (159.63 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.36%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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.

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产品名称:
Milvexian
目录号:
HY-125856
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