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BX-528

Development stage
Preclinical
Modality
Small Molecules
01

Overview

BX-528 is an experimental small molecule inhibitor developed as a potent and selective inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa). It belongs to the class of organic compounds known as phenylmethylamines. BX-528 demonstrates high selectivity for TAFIa, with an IC50 of 2 nM in enzymatic assays and 50 nM in in-vitro clot lysis assays. It shows significant selectivity over other carboxypeptidases, including CPN, CPZ, CPD, CPE (CPH), and CPB. Preclinical studies indicate that it does not significantly affect blood coagulation or platelet aggregation at high concentrations and has minimal off-target activity across a broad panel of enzymes and receptors. The compound exhibits favorable pharmacokinetics with plasma half-lives reported in animal models (0.85 hours in rats; 4.5 hours in dogs) and no significant metabolism detected across several species' hepatic microsomes[1][4][5].

Other names
BX-528BX528BX 528
02

Targets

TAFI (Carboxypeptidase B2)

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