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| | Cl-Amidine Basic information |
| Product Name: | Cl-Amidine | | Synonyms: | Cl-Amidine (trifluoroacetate salt);Cl-amidine TFA;(2S)-5-(2-Chloroethanimidamido)-2-(phenylformamido)pentanamide trifluoroacetic acid salt | | CAS: | 1043444-18-3 | | MF: | C14H19ClN4O2 ? CF3CO2H | | MW: | 424.81 | | EINECS: | | | Product Categories: | | | Mol File: | 1043444-18-3.mol |  |
| | Cl-Amidine Chemical Properties |
| storage temp. | under inert gas (nitrogen or Argon) at 2–8 °C | | solubility | ≤20mg/ml in ethanol;50mg/ml in DMSO;14mg/ml in dimethyl formamide | | form | crystalline solid |
| | Cl-Amidine Usage And Synthesis |
| Biological Activity | 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]. | | target | | Target | Value | PAD1
(Cell-free assay) | 0.8 μM | PAD4
(Cell-free assay) | 5.9 μM | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> PAD3
(Cell-free assay) 6.2 μM |
| | IC 50 | 5.9 μm | | references | [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. |
| | Cl-Amidine Preparation Products And Raw materials |
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