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Argatroban monohydrate

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Chemical Structure| 141396-28-3 同义名 : 阿加曲班单水合物 ;MD-805 monohydrate;MCI-9038 monohydrate;Argipidine monohydrate
CAS号 : 141396-28-3
货号 : A115797
分子式 : C23H38N6O6S
纯度 : 98%
分子量 : 526.649
MDL号 : MFCD00895735
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(199.37 mM)，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
动物实验配方：
生物活性
描述 Argatroban Monohydrate is a direct thrombin inhibitor synthesised to bind to the catalytic site of the thrombin molecule. It binds rapidly and reversibly to both clot-bound and soluble thrombin. Argatroban produces a predictable dose response that is well correlated with changes in anticoagulant parameters[3]. Argatroban may have a complementary effect for preventing thrombus formation without aggravating bleeding tendency because of its monotarget specificity to thrombin. Intravenous administration (0.5 to 2 micrograms/kg/min) of argatroban is a safe anticoagulant for left heart bypass in repairs of traumatic aortic rupture associated with multiple organ injuries[4]. Argatroban, as compared with heparin, appears to enhance reperfusion with TPA (tissue plasminogen activator) in patients with AMI (acute myocardial infarction), particularly in those patients with delayed presentation[5]. Intravenous argatroban improved clinical outcomes and was generally well tolerated in adults with HIT (heparin-induced thrombocytopenia) or HIT with thrombosis syndrome (HITTS). Argatroban was safe and effective for improving short and long-term outcomes in noncardioembolic stroke patients[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.49mL

1.90mL

0.95mL

18.99mL

3.80mL

1.90mL
参考文献

[1]Lyden P, Pereira B, et al. Direct thrombin inhibitor argatroban reduces stroke damage in 2 different models. Stroke. 2014 Mar;45(3):896-9.

[2]Kawai H, Yamamoto T, et al. Inhibition of factor Xa-induced platelet aggregation by a selective thrombin inhibitor, argatroban. Thromb Res. 1994 May 1;74(3):185-91.

[3]McKeage K, Plosker GL. Argatroban. Drugs. 2001;61(4):515-22; discussion 523-4

[4]Kawada T, Okada Y, Hoson M, Endo S, Yokoyama M, Kitanaka Y, Kimura K, Abe H, Yamate N. Argatroban, an attractive anticoagulant, for left heart bypass with centrifugal pump for repair of traumatic aortic rupture. Jpn J Thorac Cardiovasc Surg. 1999 Mar;47(3):104-9

[5]Jang IK, Brown DF, Giugliano RP, Anderson HV, Losordo D, Nicolau JC, Dutra OP, Bazzino O, Viamonte VM, Norbady R, Liprandi AS, Massey TJ, Dinsmore R, Schwarz RP Jr. 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 Jun;33(7):1879-85

[6]Chen S, Cai D, Huang P, Liu J, Lai Y, He J, Zhou L, Sun H. Early and long-term outcomes of argatroban use in patients with acute noncardioembolic stroke. Clin Neurol Neurosurg. 2020 Nov;198:106233