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Cl-Amidine (trifluoroacetate salt)

Catalog No.GC11032

Cl-Amidine (트리플루오로아세테이트 염)은 구강 투여 가능한 peptidylarginine deminase (PAD) 억제제로, PAD1, PAD3 및 PAD4에 대한 IC50 값은 각각 0.8 μM, 6.2 μM 및 5.9 μM입니다.

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Cl-Amidine (trifluoroacetate salt) Chemical Structure

Cas No.: 1043444-18-3

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$92.00
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1mg
US$35.00
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5mg
US$84.00
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10mg
US$133.00
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25mg
US$210.00
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50mg
US$280.00
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100mg
US$399.00
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Description Protocol Chemical Properties Product Documents Related Products

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.

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.

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