2. Metabolic Enzyme/Protease
  3. Factor Xa
  4. YM-60828 hydrochloride

YM-60828 hydrochloride 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 hydrochloride inhibits thrombus formation and platelet aggregation. YM-60828 hydrochloride can be used for the research of venous thrombosis, arterial thrombosis, and thromboembolic disorders.

For research use only. We do not sell to patients.

YM-60828 hydrochloride

YM-60828 hydrochloride Chemical Structure

CAS No. : 179755-65-8

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YM-60828 hydrochloride Related Antibodies

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Description

YM-60828 hydrochloride 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 hydrochloride inhibits thrombus formation and platelet aggregation. YM-60828 hydrochloride can be used for the research of venous thrombosis, arterial thrombosis, and thromboembolic disorders[1][2][3][4][5].

In Vitro

YM-60828 hydrochloride potently prolongs prothrombin time in pooled mouse plasma, with a CT2 value of 0.70 μM[2].
YM-60828 (3 min) hydrochloride 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 hydrochloride 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) hydrochloride dose-dependently inhibits thrombin generation in the prothrombinase complex on washed human platelet surfaces, with an IC50 of 7.7 nM[5].
YM-60828 hydrochloride 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 hydrochloride Related Antibodies
Parmacokinetics
Species Dose Route Vd CLtotal T1/2α T1/2β MRT AUC0-∞ Cmax Tmax T1/2 Bioavailability
Monkey[5] 0.3 mg/kg i.v. 0.52 L/kg 4.1 mL/min/kg 0.12 h 1.6 h 2.1 h 1220 ng·h/mL / / / /
Monkey[5] 3 mg/kg p.o. / / / / / 2475 ng·h/mL 788 ng/mL 1.0 h 1.5 h 20.3 %
In Vivo

YM-60828 (i.v.; single dose) hydrochloride dose-dependently inhibits venous thrombus formation in guinea pigs, with an ID50 of 0.012 mg/kg and significant activity at 0.03 mg/kg[1].
YM-60828 (i.v.; single dose) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride exhibits anticoagulant activity in squirrel monkeys[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR mice (male, 20-30 g)[2]
Dosage: 100 mg/kg
Administration: p.o.; single dose
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.
Animal Model: Sprague-Dawley Rats (male, 350-500 g) with carotid artery thrombus induced by occlusive thrombus[3]
Dosage: 0.1 mg/kg bolus + 0.3 mg/kg/h; 1 mg/kg bolus + 3 mg/kg/h infusion
Administration: i.v. bolus followed by continuous 1 h infusion
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.
Animal Model: Sprague-Dawley Rats (male, 350-500 g) with carotid artery thrombus induced by occlusive thrombus[4]
Dosage: 10; 30; 100 mg/kg
Administration: p.o.; single dose; 60 min pre-stimulation
Result: Dose-dependently improved carotid patency.
Occlusion rate was significantly reduced.
Duration of carotid patency was significantly increased.
Animal Model: Squirrel monkey (600-1000 g)[5]
Dosage: 0.3 (i.v.) and 3 mg/kg (p.o.)
Administration: 0.3 (i.v.) and 3 mg/kg (p.o.); single dose
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%.
Molecular Weight

610.55

Formula

C27H33Cl2N5O5S
CAS No.
SMILES

O=C(CS(=O)(N(CC1=CC2=CC(C(N)=N)=CC=C2C=C1)C3=CC=C(C=C3)OC4CCN(CC4)C(C)=N)=O)O.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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YM-60828 hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YM-60828179755-65-8YM60828YM 60828Factor XaFxathrombus formationserine proteasesfactor Xaplatelet aggregationhuman plateletsprothrombinase complexvenous thrombosisthrombinthromboembolic disordersarterial thrombosisInhibitorinhibitorinhibit

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