Argatroban


CAS No. : 74863-84-6

(Synonyms: MD-805; MCI-9038)

74863-84-6
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Cat. No. : HY-B0375
M.Wt: 508.63
Formula: C23H36N6O5S
Purity: >98 %
Solubility: DMSO : 100 mg/mL (ultrasonic)
Introduction of 74863-84-6 :

Argatroban (MD-805) is a direct, selective thrombin inhibitor. IC50 & Target:Thrombin[1]. In Vitro:Argatroban (MD-805) may have a complementary effect for preventing thrombus formation without aggravating bleeding tendency because of its monotarget specificity to thrombin. Administration (0.5 to 2 micrograms/kg/min) of Argatroban (MD-805) is a safe anticoagulant for left heart bypass in repairs of traumatic aortic rupture associated with multiple organ injuries[1]. Argatroban (MD-805), as compared with heparin, appears to enhance reperfusion with TPA in patients with AMI, particularly in those patients with delayed presentation. The incidences of major bleeding and adverse clinical outcome were lower in the patients receiving argatroban[2]. In Vivo:Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Argatroban is suitable for creating animal models to thrombolysis. In rats that have undergone hepatectomy, the pharmacokinetic parameters of Argatroban, such as the area under the curve, volume of distribution, and elimination half-life, are significantly increased. Argatroban is converted from the 21-(R) isomer to the 21-(S) enantiomer in the kidneys, which exhibits stronger antithrombotic activity and may be more readily cleared by the liver[4].

Induction of Thrombolysis[3]
Background
Argatroban is a specific thrombin inhibitor that inhibits thrombin activity in animals to establish thrombolysis models.
Specific Modeling Methods
Rat: Wistar ST • male • 8-week-old 8
Administration: 2 mg/kg/h • iv • 1 h
Note
Rats were allowed drinking water ad libitum and were fasted overnight prior to the thrombolysis experiments.
Modeling Indicators
Relative rate of thrombus dissolution ↓.
Correlated Product(s): Tranexamic acid (HY-B0149)

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