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2-cyano-Pyrimidine

カタログ番号GC11553

2-シアノ-ピリミジンは、IC50 が 170 nM の強力な非選択的システイン プロテアーゼ カテプシン K 阻害剤です。

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2-cyano-Pyrimidine 化学構造

Cas No.: 14080-23-0

サイズ 価格 在庫数 個数
1g
$9.00
在庫あり
5g
$23.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description of 2-cyano-Pyrimidine

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 of 2-cyano-Pyrimidine

Cas No. 14080-23-0 SDF
Chemical Name 2-pyrimidinecarbonitrile
Canonical SMILES NCc1ncccn1
Formula C5H3N3 M.Wt 124.1
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 20 mg/ml,PBS (pH 7.2): 3 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of 2-cyano-Pyrimidine

Prepare stock solution
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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In vivo Formulation Calculator (Clear solution) of 2-cyano-Pyrimidine

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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