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Cl-amidine hydrochloride

CAS号

1373232-26-8

分子式

C14H20Cl2N4O2

主要靶点

PAD|Apoptosis

仅限科研使用

Cat No : CM11691

Print datasheet

Synonyms

colitis|Cl amidine hydrochloride|Cl-amidine|Clamidine hydrochloride|Cl-amidine Hydrochloride|Apoptosis|inhibit|miRNA-16|miRNA|miR-16|MicroRNA|microRNA-16|Inhibitor|PAD4|Peptidylarginine Deiminase|Protein Arginine Deiminase|sepsis

验证数据展示

  • CAS No.: 1373232-26-8

    Cl-amidine hydrochloride
    CAS#: 1373232-26-8

产品信息

CAS号 1373232-26-8
分子式 C14H20Cl2N4O2
主要靶点 PAD|Apoptosis
主要通路 凋亡|表观遗传
分子量 347.24
纯度 98.14%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 colitis|Cl amidine hydrochloride|Cl-amidine|Clamidine hydrochloride|Cl-amidine Hydrochloride|Apoptosis|inhibit|miRNA-16|miRNA|miR-16|MicroRNA|microRNA-16|Inhibitor|PAD4|Peptidylarginine Deiminase|Protein Arginine Deiminase|sepsis

靶点活性

PAD4:5.9 μM

体内活性

方法：盲肠结扎和穿刺（CLP后）1小时后小鼠腹膜内给药Cl-amidine（40mg / kg），观察Cl-amidine对小鼠免受败血症诱导的致死性影响。 结果：Cl-amidine保护小鼠免受败血症诱导的致死性，同时，Cl-amidine治疗的CLP受试者动物具有更高的长期存活率。[1]

体外活性

方法：用 1 μg/mL LPS 和 10 μM Cl-脒处理小鼠原代脾细胞，处理后 6 小时收集细胞培养上清液，通过 ELISA 测定血浆和细胞培养上清液的 TNF-α以及促炎细胞因子的表达情况。 结果：Cl-amidine 血浆中TNF-α浓度下降，同时，Cl-amidine处理可显著降低这些促炎细胞因子的浓度（IL-1β，IL-6 )。[1] 方法：Cl-amidine（0，5,10,15,25,50 μg/mL, 24 小时）处理HT29和TK6 细胞，检测Cl-amidine是否可以诱导 HT29和TK6 细胞细胞凋亡。 结果：Cl-amidine以剂量依赖性方式诱导此类细胞凋亡。[2]

溶解度

DMSO:19.23 mg/mL (55.38 mM);H2O:50 mg/mL (143.99 mM)

参考文献

1.Luo Y, et al. Inhibitors and inactivators of protein arginine deiminase 4: functional and structural characterization. Biochemistry. 2006 Oct 3;45(39):11727-36.
2.Chumanevich AA, et al. Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. Am J Physiol Gastrointest Liver Physiol. 2011 Jun;300(6):G929-38.
3.Witalison EE,et al. Molecular targeting of protein arginine deiminases to suppress colitis and prevent colon cancer. Oncotarget. 2015 Nov 3;6(34):36053-62.
4.Biron BM, et al., Cl-Amidine Prevents Histone 3 Citrullination and Neutrophil Extracellular Trap Formation, and Improves Survival in a Murine Sepsis Model. J Innate Immun. 2017;9(1):22-32.

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