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2-cyano-Pyrimidine Sale

(Synonyms: 2-氰基嘧啶) 目录号 : GC11553

A cathepsin K inhibitor

2-cyano-Pyrimidine Chemical Structure

Cas No.:14080-23-0

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5g
¥473.00
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10g
¥861.00
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Sample solution is provided at 25 µL, 10mM.

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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.

Chemical Properties

Cas No. 14080-23-0 SDF
别名 2-氰基嘧啶
化学名 2-pyrimidinecarbonitrile
Canonical SMILES NCc1ncccn1
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°C
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1 mg 5 mg 10 mg
1 mM 8.058 mL 40.2901 mL 80.5802 mL
5 mM 1.6116 mL 8.058 mL 16.116 mL
10 mM 0.8058 mL 4.029 mL 8.058 mL
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