BB-Cl-Amidine

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Cat.No.:  BSM-0386
Product Name:  BB-Cl-Amidine
CAS No.:  1802637-39-3
Figure: 
Product Overview:  A PAD4 inhibitor
Description:  BB-Cl-Amidine is a modified version of Cl-amidine that retains the functional components but possesses a C-terminal benzimidazole group designed to limit proteolysis of the C-terminal amide. 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. 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. BB-Cl-Amidine is effective in vivo, improving endothelial function while downregulating the expression of type I interferon-regulated genes in MRL/lpr mice.
Appearance:  A crystalline solid
Molecular Weight:  460
Purity:  ≥95%
Storage:  -20°C
Targets:  PAD4
Molecular Formula:  C26H26ClN5O
Chemical Name:  N-[(1S)-1-(1H-benzimidazol-2-yl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-[1,1'-biphenyl]-4-carboxamide
Warning:  For Research Use Only! Not For Use in Humans.

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For Research Use Only. Not for use in diagnostic or therapeutic procedures.
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