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/ Argatroban/阿加曲班

Argatroban/阿加曲班 {[allProObj[0].p_purity_real_show]}

货号：A178436 同义名： MCI-9038; MD-805

Argatroban是一种有效的、选择性的凝血酶抑制剂，Ki值范围为5 nM至39 nM，用于抗凝研究。

Argatroban/阿加曲班 化学结构 CAS号：74863-84-6
Argatroban/阿加曲班 化学结构
CAS号：74863-84-6
Argatroban/阿加曲班 3D分子结构
CAS号：74863-84-6
Argatroban/阿加曲班 化学结构 CAS号：74863-84-6
Argatroban/阿加曲班 3D分子结构 CAS号：74863-84-6
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Argatroban/阿加曲班 纯度/质量文件 产品仅供科研

货号：A178436 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 Thrombin ↓ 其他靶点 纯度
Dabigatran +++

Thrombin, IC50: 9.3 nM

 		98%
Dabigatran etexilate ✔ 98%
Argatroban 99%+
Heparin sodium salt ✔ ≥150 u/mg
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Argatroban/阿加曲班 生物活性

靶点

  • Thrombin

    Thrombin, Ki:5-39 nM
描述 Argatroban (MD-805), targeting thrombin specifically, offers a beneficial approach to thrombus prevention without increasing the risk of bleeding. It is administered at a rate of 0.5 to 2 micrograms/kg/min as a safe anticoagulant during left heart bypass procedures for traumatic aortic ruptures accompanied by multiple organ injuries[1]. Comparatively, Argatroban (MD-805) enhances the effectiveness of reperfusion treatments with TPA in patients with acute myocardial infarction (AMI), especially those with delayed presentations. Clinical trials indicate that both major bleeding incidents and adverse clinical outcomes are less frequent in patients treated with Argatroban than those receiving heparin[2].
体外研究

Argatroban (MD-805), targeting thrombin specifically, offers a beneficial approach to thrombus prevention without increasing the risk of bleeding. It is administered at a rate of 0.5 to 2 micrograms/kg/min as a safe anticoagulant during left heart bypass procedures for traumatic aortic ruptures accompanied by multiple organ injuries[1].

Comparatively, Argatroban (MD-805) enhances the effectiveness of reperfusion treatments with TPA in patients with acute myocardial infarction (AMI), especially those with delayed presentations. Clinical trials indicate that both major bleeding incidents and adverse clinical outcomes are less frequent in patients treated with Argatroban than those receiving heparin[2].

Argatroban/阿加曲班 细胞实验

Cell Line
Concentration Treated Time Description References
PC-3 10 µM, 50 µM, 100 µM 24 h To evaluate the inhibitory effect of Argatroban on the E2F1:MTA1 complex and its impact on HAS2 expression. Results showed that Argatroban significantly reduced HAS2 transcript and protein levels without affecting E2F1 and MTA1 expression. Theranostics. 2019 Feb 20;9(5):1490-1509.
SK-Mel-147 10 µM, 50 µM, 100 µM 24 h To evaluate the inhibitory effect of Argatroban on the E2F1:MTA1 complex and its impact on HAS2 expression. Results showed that Argatroban significantly reduced HAS2 transcript and protein levels without affecting E2F1 and MTA1 expression. Theranostics. 2019 Feb 20;9(5):1490-1509.
Murine lung epithelial cells 100 nM Argatroban inhibited Morf4l1-dependent histone acetylation, reduced its cytotoxicity, and improved survival of mice with experimental lung injury at doses that had no anticoagulant activity. Sci Transl Med. 2015 Oct 28;7(311):311ra171.
Platelets 0.4-16 μg/mL 30 minutes To evaluate the effect of Argatroban on VITT IgG binding to PF4, results showed Argatroban at therapeutic concentrations did not significantly inhibit VITT IgG binding to PF4 Blood Adv. 2024 Nov 26;8(22):5744-5752.

Argatroban/阿加曲班 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
NMRI nude mice Melanoma metastasis model Intraperitoneal injection 9 mg/kg Every other day for 4 weeks To evaluate the inhibitory effect of Argatroban on melanoma metastasis in vivo. Results showed that Argatroban significantly reduced the formation of lung metastases and decreased HAS2 expression and infiltration of tumor-associated macrophages. Theranostics. 2019 Feb 20;9(5):1490-1509.
Mice Experimental pneumonia model Intratracheal 5 µg/mouse Single dose, for 24 hours Argatroban inhibited Morf4l1-dependent histone acetylation, reduced its cytotoxicity, and improved survival of mice with experimental lung injury at doses that had no anticoagulant activity. Sci Transl Med. 2015 Oct 28;7(311):311ra171.
DdY mice Oxaliplatin-induced peripheral neuropathy model Intraperitoneal injection 10 mg/kg Single administration To evaluate the impact of thrombin inhibitor on TMα's anti-neuropathic activity J Neuroinflammation. 2019 Oct 30;16(1):199.
Mice K/BxN transgenic mice and serum transfer-induced arthritis (STIA) model Ex vivo co-incubation 350 µM Single treatment Argatroban inhibited the fluorescence signal of RACPP NleTPRSFL, indicating that it reduced probe cleavage by inhibiting thrombin activity. Arthritis Rheumatol. 2018 Jan;70(1):69-79
C57BL/6J mice Carotid artery thrombolysis stroke model (iCAT) Intravenous 80 mg/kg bolus; 40 mg/kg/min infusion over 60 minutes Single administration, duration of 60 minutes To evaluate the effect of argatroban combined with rtPA on thrombolysis and recanalization. Results showed that argatroban increased recanalization rates to 50%, but also increased carotid artery embolization and stroke-related mortality. Blood Adv. 2022 Sep 27;6(18):5449-5462
Mice VITT mouse model Osmotic pump 120 μg/kg/h Continuous infusion To assess the effect of Argatroban on thrombosis in VITT mice, results showed Argatroban significantly reduced clot formation but did not ameliorate thrombocytopenia Blood Adv. 2024 Nov 26;8(22):5744-5752.
Mice Bleomycin-induced pulmonary fibrosis model Intraperitoneal injection 9 mg/kg Daily for 14 days Argatroban significantly improved the survival of PN-1?/? mice by inhibiting thrombin activity, reducing the accumulation of inflammatory cells and platelets in the lungs. Blood Adv. 2018 Sep 25;2(18):2389-2399

Argatroban/阿加曲班 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00603824 Heparin-Induced Thrombocytopen... 展开 >>ia 收起 << Phase 4 Withdrawn(PI relocated) - -
NCT01911624 Staphylococcus Aureus Bacterae... 展开 >>mia 收起 << Phase 2 Completed - Belgium ... 展开 >> KUleuven/UZ Gasthuisberg Leuven, Belgium, 3000 收起 <<
NCT00921856 Coronary Vasospasm ... 展开 >> Microvascular Angina Coronary Artery Disease 收起 << Not Applicable Recruiting December 2019 Germany ... 展开 >> Robert Bosch Medical Center Recruiting Stuttgart, Germany, 70376 Contact: Peter Ong, MD    +4971181016048    petereong@gmail.com    Contact: Anastasios Athanasiadis, MD    +4971181015444 收起 <<

Argatroban/阿加曲班 参考文献

[1]Kawada, T., et al., Argatroban, an attractive anticoagulant, for left heart bypass with centrifugal pump for repair of traumatic aortic rupture. Jpn J Thorac Cardiovasc Surg, 1999. 47(3): p. 104-9.

[2]Jang, I.K., et al., A multicenter, randomized study of argatroban versus heparin as adjunct to tissue plasminogen activator (TPA) in acute myocardial infarction: myocardial infarction with novastan and TPA (MINT) study. J Am Coll Cardiol, 1999. 33(7): p. 1879-85.

Argatroban/阿加曲班 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.83mL

1.97mL

0.98mL

19.66mL

3.93mL

1.97mL

Argatroban/阿加曲班 技术信息

CAS号74863-84-6
分子式C23H36N6O5S
分子量 508.63
SMILES Code O=C([C@@H]1N(C([C@@H](NS(=O)(C2=CC=CC3=C2NCC(C)C3)=O)CCCNC(N)=N)=O)CC[C@@H](C)C1)O
MDL No. MFCD23102419
别名 MCI-9038; MD-805; Argipidine
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C
溶解方案

DMSO: 105 mg/mL(206.44 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Argatroban | 74863-84-6 | MD-805 | MCI-9038 | Argipidine | MD805 | MD 805 | MCI9038 | MCI 9038 | MCI-9038 | Thrombin Inhibitor | Induced Disease Models Products | Metabolic Enzyme/Protease | Cardiovascular System Disease Models | Thrombin | Thrombolysis Models | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Argatroban/阿加曲班 纯度/质量文件 | Argatroban/阿加曲班 亚型比较 | Argatroban/阿加曲班 生物活性 | Argatroban/阿加曲班 临床数据 | Argatroban/阿加曲班 参考文献 | Argatroban/阿加曲班 实验方案 | Argatroban/阿加曲班 技术信息

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