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Cl-amidine

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Chemical Structure| 913723-61-2 同义名 : -
CAS号 : 913723-61-2
货号 : A285695
分子式 : C14H19ClN4O2
纯度 : 98+%
分子量 : 310.779
MDL号 : MFCD20278255
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 PAD4 (protein arginine deiminase 4) is a transcriptional coregulator that catalyzes the calcium-dependent conversion of specific arginine residues in proteins to citrulline. Cl-amidine is a first-generation irreversible PADs inhibitor with IC50 values of 0.8, 17, 6 and 5.9μM for PAD1, PAD2, PAD3 and PAD4, respectively. Cl-amidine at concentration ranging in 25-200μM dose-dependently inhibited the PAD4-mediated enhancement of the p300GBD-GRIP1 interaction in CV-1 cells post 40-hour treatment. Cl-amidine at concentration of 100μM significantly reduced the level of citrullinated histone H3 induced by A23187 in HL-60 granulocytes. Administration of 40mg/kg Cl-amidine, i.p., exhibited protective effect on CLP (cecal ligation and puncture)-induced lethal septic shock in mice asi it significantly decreased BM and thymus atrophy, restored innate immune cells in BM, increased blood monocytes and blood/liver bacteria clearance and attenuated pro-inflammatory cytokine production.
作用机制 Cl-amidine specifically inactivates PAD4 by modifying Cys645.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.22mL

0.64mL

0.32mL

16.09mL

3.22mL

1.61mL

32.18mL

6.44mL

3.22mL
参考文献

[1]Luo Y, Arita K, et al. Inhibitors and inactivators of protein arginine deiminase 4: functional and structural characterization. Biochemistry. 2006 Oct 3;45(39):11727-36.

[2]Causey CP, Jones JE, et al. The development of N-α-(2-carboxyl)benzoyl-N(5)-(2-fluoro-1-iminoethyl)-l-ornithine amide (o-F-amidine) and N-α-(2-carboxyl)benzoyl-N(5)-(2-chloro-1-iminoethyl)-l-ornithine amide (o-Cl-amidine) as second generation protein arginine deiminase (PAD) inhibitors. J Med Chem. 2011 Oct 13;54(19):6919-35.

[3]Zhao T, Pan B, et al. Protective effect of Cl-amidine against CLP-induced lethal septic shock in mice. Sci Rep. 2016 Nov 7;6:36696.