Name: Cl-Amidine (trifluoroacetate salt)
Price: 312.00 USD

- Overview
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    Background
    
    IC50: 5.9 μM
    Cl-Amidine is a PAD4 deimination activity inhibitor.
    Protein arginine deiminase 4 (PAD4) can catalyze the post-translational modification of arginine residues on histones to form citrulline, which can change gene expression. Thus, dysregulated PAD4 activity has been implicated in cancer and rheumatoid arthritis.
    In vitro: Previous study found that Cl-amidine antagonized the PAD4-mediated enhancement of the the p300GBD-GRIP1 interaction dose-dependently, and it was noteworthy that Cl-amidine treatment had only a minimal reduction in the efficiency of the interaction in Cys645S-transfected cells, thereby suggesting that the inhibitory effect of Cl-amidine was not a nonspecific one but was targeted at the active PAD4 enzyme. These results demonstrated that Cl-amidine was significantly more potent than F-amidine, consistent with its improved in vitro potency [1].
    In vivo: Animal study showed that Cl-amidine could improve survival in a mouse model of cecal ligation and puncture (CLP)-induced septic shock. Cl-amidine was proven to play protective roles by restoring innate immune cells in BM, decreasing BM and thymus atrophy, increasing blood monocytes and blood/liver bacteria clearance, and attenuating pro-inflammatory cytokine production in a murine lethal sepsis model [2].
    Clinical trial: So far, no clinical study has been conducted.
    
    [1] Luo, Y. ,Arita, K.,Bhatia, M., et al. Inhibitors and inactivators of protein arginine deiminase 4: Functional and structural characterization. Biochemistry 45(39), 11727-11736 (2006).
    [2] Zhao T, Pan B, Alam HB, Liu B, Bronson RT, Deng Q, Wu E, Li Y. Protective effect of Cl-amidine against CLP-induced lethal septic shock in mice. Sci Rep. 2016 Nov 7;6:36696.
- Properties
  - Alternative Name
    
    N-[(1S)-1-(aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide 2,2,2-trifluoroacetate
    
    CAS Number
    
    1043444-18-3
    
    Molecular Formula
    
    C14H19ClN4O2·CF3CO2H
    
    Molecular Weight
    
    424.8
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    Purity ≥95.00%
    
    Solubility
    
    ≤20mg/ml in ethanol;50mg/ml in DMSO;14mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Cl-Amidine (trifluoroacetate salt)

Cl-Amidine (trifluoroacetate salt)

Background

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