| CAS NO: | 1043444-18-3 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 424.8 |
| Cas No. | 1043444-18-3 |
| Formula | C14H19ClN4O2·CF3CO2H |
| Solubility | ≤20mg/ml in ethanol;50mg/ml in DMSO;14mg/ml in dimethyl formamide |
| Chemical Name | N-[(1S)-1-(aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide 2,2,2-trifluoroacetate |
| Canonical SMILES | O=C(N[C@@H](CCCNC(CCl)=N)C(N)=O)C1=CC=CC=C1.FC(F)(C(O)=O)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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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