product name Argatroban
Description: Argatroban (also known as MCI-9038) is a potent and selective synthetic thrombin inhibitor with Ki ranging from 5 nM to 39 nM. Argatroban is used as an anticoagulant that acts as a direct thrombin inhibitor. Argatroban received FDA approval in 2000 for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT). As a direct thrombin inhibitor, Argatroban reversibly binds to the thrombin active site. Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions which include fibrin formation, activation of coagulation factors V, VIII, and XIII; activation of protein C, and platelet aggregation as well.
References: Br J Pharmacol. 1994 Dec;113(4):1209-14; Jpn J Pharmacol. 1995 Oct;69(2):143-8.
508.63
Formula
C23H36N6O5S
CAS No.
74863-84-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 9 mg/mL (17.7 mM)
Water: <1 mg/mL
Ethanol: 6 mg/mL (11.8 mM)
Solubility (In vivo)
Synonyms
MCI-9038
other peoduct :
| In Vitro |
In vitro activity: Argatroban is a potent and selective synthetic thrombin inhibitor with Ki values against thrombin ranging from 5 nM to 39 nM. Argatroban has antithrombotic properties in a wide variety of animal models of both platelet-rich and erythrocyte-rich thrombosis. Argatroban dose-dependently prevents thrombus formation with an estimated ED50 of 125 μg/kg in this test. Argatroban produces a dose-dependent increases in the thrombin time with a 511% increase at the highest dose used with only a 73% increase in the APTT at this dose. Argatroban can directly induce phenotype conversion of vascular smooth muscle cells with the resultant up-regulation of SMemb, PAI-1, and beta-actin mRNAs. Kinase Assay: Cell Assay: |
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| In Vivo | Argatroban inhibits the formation of microthrombi up to 3 hours after middle cerebral artery (MCA) occlusion; beyond 3 hours, it is ineffective. Argatroban also significantly reduces the size of ischemic cerebral lesions at 6 hours after MCA occlusion. Argatroban (0.3 mg/h/rat) significantly decreases the number of microthrombi 1 day after distal middle cerebral artery (dMCA) occlusion in the rat distal middle cerebral artery occlusion model. Argatroban (0.1 and 0.3 mg/h/rat) significantly reverses a decrease in regional cerebral blood flow (rCBF) 1 day after distal middle cerebral artery (dMCA) occlusion. Argatroban (0.3 mg/h/rat) also significantly reduces the size of the cerebral infarction. |
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| References | Br J Pharmacol. 1994 Dec;113(4):1209-14; Jpn J Pharmacol. 1995 Oct;69(2):143-8. |
