YM-60828 methanesulfonate
YM-60828 methanesulfonate is an orally active, selective and competitive factor Xa inhibitor with a Ki of 1.3 nM and an IC50 of 2.3 nM. YM-60828 methanesulfonate inhibits thrombus formation and platelet aggregation. YM-60828 methanesulfonate can be used for the research of venous thrombosis, arterial thrombosis, and thromboembolic disorders.
For research use only. We do not sell to patients.
- CAS No.: 209187-02-0
- Formula: C28H35N5O8S2
- Molecular Weight:633.74
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
YM-60828 methanesulfonate potently prolongs prothrombin time in pooled mouse plasma, with a CT2 value of 0.70 μM[2].
YM-60828 (3 min) methanesulfonate dose-dependently prolongs human plasma factor Xa clotting time, prothrombin time, and activated partial thromboplastin time, with CT2 values of 0.10 μM, 0.21 μM, and 0.24 μM respectively, and does not affect thrombin time at concentrations up to 100 μM[5].
YM-60828 methanesulfonate dose-dependently prolongs prothrombin time and activated partial thromboplastin time in plasma from multiple species, with the highest potency in squirrel monkey plasma (CT2 0.16 μM for PT, 0.18 μM for APTT) and lowest potency in guinea pig plasma (CT2 2.79 μM for PT, 1.36 μM for APTT)[5].
YM-60828 (0.1-100 nM) methanesulfonate dose-dependently inhibits thrombin generation in the prothrombinase complex on washed human platelet surfaces, with an IC50 of 7.7 nM[5].
YM-60828 methanesulfonate dose-dependently inhibits agonist-induced aggregation of human platelets, with IC50 values ranging from 3.3 μM (TRAP-induced in PRP) to 23.4 μM (Thrombin-induced in washed platelets)[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
YM-60828 (i.v.; single dose) methanesulfonate dose-dependently inhibits thrombus formation in a guinea pig arterio-venous shunt model, with an ID50 of 0.0094 mg/kg and significant activity at 0.01 mg/kg[1].
YM-60828 (i.v.; single dose) methanesulfonate dose-dependently inhibits carotid artery thrombus formation in guinea pigs, with an ID50 of 0.14 mg/kg and significant activity at 0.3 mg/kg[1].
YM-60828 (100 mg/kg; p.o.; single dose) methanesulfonate exhibits anticoagulant activity in ICR mice[2].
YM-60828 (0.1-1 mg/kg bolus + 0.3-3 mg/kg/h infusion; i.v.; 60 min) methanesulfonate dose-dependently improves carotid artery patency after moPA-induced thrombolysis in rats with electrically-induced arterial thrombosis[3].
YM-60828 (10-100 mg/kg; p.o.; single dose; 60 min pre-stimulation) methanesulfonate improves carotid artery patency in a rat arterial thrombosis model[4].
YM-60828 (0.3 (i.v.) and 3 mg/kg (p.o.); single dose) methanesulfonate exhibits anticoagulant activity in squirrel monkeys[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (male, 20-30 g)[2]
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Dosage:100 mg/kg
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Administration:p.o.; single dose
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Result:Prolonged prothrombin time to 2.6-fold relative to control at 0.5 hours post-administration.
Prolonged prothrombin time to 1.7-fold relative to control at 2.0 hours post-administration.
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Animal Model:Sprague-Dawley Rats (male, 350-500 g) with carotid artery thrombus induced by occlusive thrombus[3]
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Dosage:0.1 mg/kg bolus + 0.3 mg/kg/h; 1 mg/kg bolus + 3 mg/kg/h infusion
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Administration:i.v. bolus followed by continuous 1 h infusion
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Result:Increased duration of patency relative to moPA-only controls.
Achieved 8/8 reperfusion rate, 5/8 reocclusion rate, and increased duration of patency relative to moPA-only controls.
Achieved 8/8 reperfusion rate, 50% reocclusion rate, and significantly increased duration of patency relative to moPA-only controls.
Dose-dependently increased blood loss but not significantly different from moPA-only controls.
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Animal Model:Sprague-Dawley Rats (male, 350-500 g) with carotid artery thrombus induced by occlusive thrombus[4]
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Dosage:10; 30; 100 mg/kg
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Administration:p.o.; single dose; 60 min pre-stimulation
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Result:Dose-dependently improved carotid patency.
Occlusion rate was significantly reduced.
Duration of carotid patency was significantly increased.
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Animal Model:Squirrel monkey (600-1000 g)[5]
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Dosage:0.3 (i.v.) and 3 mg/kg (p.o.)
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Administration:0.3 (i.v.) and 3 mg/kg (p.o.); single dose
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Result:Prolonged PT by 4.8-fold and APTT by 1.9-fold at 1 hour after oral administration of 3 mg/kg.
Peaked anticoagulant activity at 1-2 hours and returned to baseline by 8 hours post-oral administration.
Reached maximum plasma concentration of 788 ng/mL at 1 hour after oral administration of 3 mg/kg.
Reached plasma drug concentration of 894 ng/mL at 5 minutes after intravenous administration of 0.3 mg/kg.
Exhibited early-phase half-life of 0.12 hours and terminal-phase half-life of 1.6 hours after intravenous administration of 0.3 mg/kg.
Achieved oral bioavailability of 20.3%.
Chemical Information
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CAS No. 209187-02-0
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Molecular Weight 633.74
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Formula C28H35N5O8S2
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SMILES
O=S(N(CC1=CC=C2C=CC(C(N)=N)=CC2=C1)C(C=C3)=CC=C3OC4CCN(CC4)C(C)=N)(CC(O)=O)=O.O=S(O)(C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Sato K, et al. Relationship between the antithrombotic effect of YM-75466, a novel factor Xa inhibitor, and coagulation parameters in rats. Eur J Pharmacol. 1998 Apr 24;347(2-3):231-6. [Content Brief]
[2]. Hirayama F, et al. The discovery of YM-60828: a potent, selective and orally-bioavailable factor Xa inhibitor. Bioorg Med Chem. 2002;10(5):1509-1523. [Content Brief]
[3]. Kawasaki T, et al. Effect of a synthetic factor Xa inhibitor, YM-60828, on blood vessel patency in combination with a thrombolytic agent and on blood loss from the operation site in a rat model of arterial thrombosis. Thromb Haemost. 1998;79(4):859-864. [Content Brief]
[4]. Kawasaki T, et al. Comparative studies of an orally-active factor Xa inhibitor, YM-60828, with other antithrombotic agents in a rat model of arterial thrombosis. Thromb Haemost. 1998;79(2):410-416. [Content Brief]
[5]. Taniuchi Y, et al. Biochemical and pharmacological characterization of YM-60828, a newly synthesized and orally active inhibitor of human factor Xa. Thromb Haemost. 1998;79(3):543-548. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YM-60828 methanesulfonate Related Classifications
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