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Cat. No. Product Name CAS No. Information
PC-60957

LY-517717

313489-71-3

A potent, selective, and orally bioavailable factor Xa (FXa) inhibitor for prevention and treatment of thromboembolic diseases.

Thrombosis

Phase 2 Clinical

PC-60548

BMS-986120

1478712-37-6

BMS-986120 (BMS986120) is a potent, selective, orally bioavailable, and reversible PAR4 antagonist with Kd of 0.098 nM for human PAR4; selectivity inhibits PAR4 AP-induced cellular calcium mobilization in HEK cells with IC5o of 0.56 nM, with no activity on PAR1 and PAR2; inhibits human PRP aggregation in response to γ-thrombin in vitro with IC50 of 7.3 nM; demonstrates potent and highly efficacious antithrombotic activity with low bleeding in vivo.

Thrombosis

Phase 2 Clinical

PC-63359

Letaxaban

870262-90-1 Letaxaban (TAK-442, TAK442) is a potent, selective and direct factor Xa (FXa) inhibitor with Ki of 1.8 nM for hFXa, >440-fold selectivity than thrombin and negligible effects on trypsin, plasmin, and tPA; In human plasma, TAK-442 doubles FXa-induced clotting time, prothrombin time (PT), and activated partial thromboplastin time at 0.19, 0.55, and 0.59 uM, respectively; demonstrates antithrombotic effects in rabbit model of venous thrombosis.

Thrombosis

Phase 2 Discontinued

PC-63163

AZD-0837

433937-93-0 AZD-0837 is a novel oral anticoagulant that after bioconversion to its active form is a potent and reversible thrombin inhibitor, has been investigated in phase II studies for prevention of stroke and systemic embolic events in patients with atrial fibrillation (AF).

Thrombosis

Phase 2 Discontinued

PC-62457

XR 5118

174766-49-5 XR 5118 is a small molecule plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 3.5 uM, binds to PAI-1 and reduces plasma PAI-1 activity levels, promotes endogenous thrombolysis and inhibits thrombus accretion; the first nonpeptide compound with significant anti-PAI-1 activity in vivo.

Thrombosis

Discontinued

PC-62046

YM-254890

568580-02-9 YM 254890 is a selective Gq signaling inhibitor that strongly inhibits intracellular calcium ion mobilization and serum response element (SRE)-mediated transcription stimulated by several receptors coupled to Gq, but not those coupled to Gi, Gs, or G15; also exhibits antithrombotic and thrombolytic effects in an electrically induced carotid artery thrombosis model in rats; inhibits ADP-induced platelet aggregation in human platelet-rich plasma with an IC50 of <0.6 uM by blocking the P2Y1 receptor-signal transduction pathway.

Thrombosis

Discontinued

PC-62006

BMS-962212

1430114-34-3 BMS-962212 is a potent, highly selective and reversible small molecule coagulation Factor XIa (FXIa) inhibitor with Ki of 0.7 nM; displays an excellent protease selectivity profile, including thrombin, Factor Xa/VIIa/IXa/XIIa, plasma or tissue kallikrein; shows excellent preclinical efficacy in thrombosis models and aqueous solubility suitable for intravenous administration.

Thrombosis

Phase 1 Clinical

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