Darexaban|365462-23-3|(YM150)-陌孚医药/Medlife

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Darexaban (Synonyms: YM150)

目录号: PL11222 纯度: ≥99%

CAS No. :365462-23-3

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中文名称	Darexaban
中文别名	N-[2-羟基-6-(4-甲氧基苯甲酰氨基)苯基]-4-(4-甲基-1,4-二氮杂庚烷-1-基)苯甲酰胺;Darexaban标准品;N-[2-羟基-6-(4-甲氧基苯酰胺)苯基]-4-(4-甲基-1,4-二氮杂环庚烷-1-基)苯甲酰胺
英文名称	Darexaban
英文别名	N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide;N-[2-hydroxy-6-[(4-methoxybenzoyl)amino]phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide;TANEXABAN;Darexaban
Cas No.	365462-23-3
分子式	C₂₇H₃₀N₄O₄
分子量	474.55
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Darexaban (YM150) 是一种有效、选择性和具有口服活性的 Xa 因子 (FXa) 抑制剂，IC₅₀ 为 54.6 nM。Darexaban 对其他相关丝氨酸蛋白酶（如胰蛋白酶、凝血酶和激肽释放酶）显示出高选择性。Darexaban 具有抗凝和抗血栓形成作用。

生物活性

Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC 50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects.

性状

Solid

体外研究(In Vitro)

Darexaban is an oral direct factor Xa (FXa) inhibitor that is rapidly and extensively metabolized into its glucuronide conjugate (YM-222714) post-administration. Darexaban competitively and selectively inhibits human FXa, and also inhibits the prothrombin activation induced by prothrombinase complex or whole blood clot with similar potency to free FXa. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

In mice, Darexaban inhibits FXa activity in plasma with an ED 50 value of 24.8 mg/kg. Darexaban prolonges prothrombin time (PT) at 3 mg/kg.
In a pulmonary thromboembolism (PE) mouse model, Darexaban dose-dependently reduces the mortality rate, significantly so at 10 mg/kg.
In a FeCl3-induced venous thrombosis (VT) mouse model, Darexaban (0.3-10 mg/kg) dose-dependently decreases the thrombus protein content, significantly so at doses of 3 mg/kg or higher.
has not independently confirmed the accuracy of these methods. They are for reference only.

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

ClinicalTrial

参考文献

[1]. Fukushi Hirayama, et al. Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. J Med Chem. 2011 Dec 8;54(23):8051-65.
[2]. Seiji Kaku, et al. Darexaban: anticoagulant effects in mice and human plasma in vitro, antithrombotic effects in thrombosis and bleeding models in mice and effects of anti-inhibitor coagulant complex and recombinant factor VIIa. Thromb Res. 2013 May;131(5

溶解度数据	In Vitro: DMSO : 250 mg/mL (526.81 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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