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Garadacimab

CAS No. : 2162134-62-3

產(chǎn)品活性：Garadacimab (CSL312) is a first-in-class, fully human IgG4 monoclonal antibody targeting activated factor XII (FXIIa). Garadacimab has the potential for hereditary angioedema research.

研究領(lǐng)域：Metabolic Enzyme/Protease

作用靶點(diǎn)：Factor Xa

In Vitro: Garadacimab (CSL312) displays high affinity to activated βFXIIa with a K_D of 140 pM and shows potency in an activated partial thromboplastin time (aPTT) assay with human plasma. Garadacimab shows high selectivity over a panel of relevant human serine proteases (FVIIa, FIXa, FXa, FXIa, kallikrein, tissue plasminogen activator, activated protein C, and urokinase plasminogen activator).

In Vivo: In male and female cynomolgus monkeys, Garadacimab (0.5, 1, and 3 mg/kg i.v. and 6 and 20 mg/kg s.c. over 8 weeks) plasma concentrations increased in a dose-dependent manner.
Garadacimab has an inhibitory effect on FXII-mediated kallikrein activity. Furthermore, Garadacimab causes a clear dose-dependent prolongation of activated partial thromboplastin time (aPTT) with no associated effect on the prothrombin time.

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