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2-cyano-Pyrimidine
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。
2-cyano-Pyrimidine图片
CAS NO:14080-23-0
包装与价格:
包装价格(元)
5g电议
10g电议

产品介绍
2-cyano-Pyrimidine 是一种有效的非选择性半胱氨酸蛋白酶组织蛋白酶 K 抑制剂,IC50 为 170 nM。
Cas No.14080-23-0
别名2-氰基嘧啶
化学名2-pyrimidinecarbonitrile
Canonical SMILESNCc1ncccn1
分子式C5H3N3
分子量124.1
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 20 mg/ml,PBS (pH 7.2): 3 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 170 nM

2-cyano-Pyrimidine is a cathepsin K inhibitor.

Cathepsin K is a protease defined by its high specificity for kinins, which is involved in bone resorption. Cathepsin K's ability to catabolize collagen, elastin, and gelatin allow it to break down bone and cartilage. Such catabolic activity is also partially responsible for the loss of lung elasticity and recoil in emphysema. Therefore, inhibitors of Cathepsin K are showing great potential in the treatment of osteoporosis.

In vitro: 2-cyano-Pyrimidine was identified as a cathepsin K inhibitor whose basic structure and derivatives have been evaluated for the treatment of osteoporosis. Enzymatic study showed that 2-cyano-Pyrimidine had an IC50 value of 170 nM for inhibition of cathepsin K, elevated activity of which has been linked to the formation of osteoporosis and arthritis. Moreover, Cathepsin K was found to be a lysosomal cysteine protease found in osteoclasts. [1,2].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Altmann, E. ,Aichholz, R.,Betschart, C., et al. 2-cyano-pyrimidines: A new chemotype for inhibitors of the cysteine protease cathepsin K. Journal of Medicinal Chemistry 50(4), 591-594 (2007).
[2] Rankovic Z et al.  Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1524-7.