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Cl-Amidine(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cl-Amidine(hydrochloride)图片
CAS NO:1373232-26-8
规格:98%
分子量:347.2
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
Cl-amidine is an inhibitor of protein arginine deiminases (PAD; IC50s = 0.8, 6.2, and 5.9 uM for PAD1, PAD3, and PAD4 in vitro, respectively).
CAS:1373232-26-8
分子式:C14H19ClN4O2.HCl
分子量:347.2
纯度:98%
存储:Store at -20°C

Background:

Cl-amidine (hydrochloride) is a peptidylarginine deminase (PAD) inhibitor, with an IC50 5.9 μM for PAD4.


Cl-amidine is a peptidylarginine deminase (PAD) inhibitor, with an IC50 of 5.9±0.3 μM for PAD4 and Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000 M-1.min-1 for PAD4)[1]. Cl-amidine induces apoptosis (identified as annexin V-positive/propidium iodide-negative cells) in such cells in a dose-dependent manner, indicating that Cl-amidine induces apoptosis of WBCs in vitro. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine[2].


Significantly higher levels of colon inflammation in the 2% DSS than the 2% DSS+Cl-amidine mice are showed. The mean histology scores are 24.2±1.7 (SE) and 13.9±1.6, respectively. Most of the damage in the DSS-only group is in the distal colon, and this damage is suppressed with DSS+Cl-amidine. For the DSS-treated group, the mean colon length is 7.2±0.2 cm. In contrast, the average colon length of the DSS+Cl-amidine group is 8.4±0.2 cm, which is comparable to the mean colon lengths obtained for the wateralone and water+Cl-amidine groups (8.4±0.3 and 7.9±0.2 cm, respectively). The total distance and average speed of mice over a 96-h period are also measured. The results of these analyses demonstrate that the total distance is 5,072±381 and 3,190±401 m for the water-treated and DSS+Cl-amidine mice, but only 800±163 m for the DSS-only group. Similarly, the average speed on the wheel over the 4-day period is 6.2±0.63 and 5.3±0.58 m/min for the water-treated and DSS+Cl-amidine groups, but only 1.8±0.51 m/min for the DSS group[2].


参考文献:
[1]. Yuan Luo, et al. Inhibitors and Inactivators of Protein Arginine Deiminase 4: Functional and Structural Characterization. Biochemistry. 2006 Oct 3; 45(39): 11727–11736.
[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.