BB-Cl-Amidine

BB-Cl-Amidine

CAT N°: 17079
Price:

102.00 86.70

BB-Cl-Amidine is a modified version of Cl-amidine (Item No. 10599) that retains the functional components but possesses a C-terminal benzimidazole group designed to limit proteolysis of the C-terminal amide.{27726} BB-Cl-Amidine irreversibly inactivates all four PAD subtypes (kinact/KI = 16,100, 4,100, 6,800, and 13,300 M-1min-1 for PAD1-4, respectively) by covalently modifying an active site cysteine that is important for its catalytic activity.{18132,36047} The cellular potency of BB-Cl-amidine against PAD4 is increased 20-fold over the parent compound (EC50 = 8.8 µM versus >200 µM for Cl-amidine). BB-Cl-Amidine also has a significantly longer in vivo half-life than Cl-amidine (1.75 h versus ~15 min, respectively). Both compounds inhibit the formation of neutrophil extracellular traps without altering H2O2 production by neutrophils.{27726} BB-Cl-Amidine is effective in vivo, improving endothelial function while downregulating the expression of type I interferon-regulated genes in MRL/lpr mice.

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