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Cathepsin Inhibitor 1
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。
Cathepsin Inhibitor 1图片
CAS NO:225120-65-0
包装:5mg
市场价:2610元

产品介绍
Cathepsin inhibitor 1 (compound 25) 是一种有效的选择性 Cathepsin 抑制剂,对 CatL、CatL2、CatS、CatK 和 CatB 的 pIC50 分别为 7.9、6.7、6.0、5.5 和 5.2。
Cas No.225120-65-0
化学名5-tert-butyl-N-[(2S)-3-(3-chlorophenyl)-1-(cyanomethylamino)-1-oxopropan-2-yl]-2-methylpyrazole-3-carboxamide
Canonical SMILESCC(C)(C)C1=NN(C(=C1)C(=O)NC(CC2=CC(=CC=C2)Cl)C(=O)NCC#N)C
分子式C20H24ClN5O2
分子量401.89
溶解度Soluble in DMSO
储存条件Store at -20°C
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

pIC50: 7.9, 6.7, 6.0, 5.5 and 5.2 for Cathepsin (L, L2, S, K, B), respectively

Cathepsin Inhibitor 1 is an inhibitor of Cathepsin. Osteoarthritis is currently recognized as a chronic degenerative disease, which is caused by the loss of articular cartilage and damage to underlying bone, resulting in joint instability and pain. The lysosomal cysteine protease2 Cathepsin L (CatL) is found to be a potential target for intervention in treatment of osteoarthritis. After secreted into the extracellular matrix, CatL can degrade proteoglycans such as aggrecan4 and type II collagen, which are the major components of articular cartilage.

In vitro: The CatL pIC50 value of Cathepsin Inhibitor 1 was found to exceed that of its analog by 1.6 units. Moreover, CatS (ΔpIC50 = -0.1) and CatL2 (ΔpIC50 = 0.5) were much less sensitive to the structural change of Cathepsin Inhibitor 1, leading to an improved selectivity profile relative to its analog. Cathepsin Inhibitor 1 was as least as selective with respect to CatB and CatS as previously described CatL inhibitors. The crystal structure of its another analog bound to CatL provided the rationale for the SAR observed for Cathepsin Inhibitor 1. The 1-methyl group of the pyrazole made some contact with Leu69 and appeared to force the pyrazole ring out of co-planarity with the amide, likely functioning as a conformational lock [1].

In vivo: So far, there is no in vivo animal data available for Cathepsin Inhibitor 1 is an inhibitor of Cathepsin.

Clinical trial: N/A

Reference:
[1] Asaad N, Bethel PA, Coulson MD, Dawson JE, Ford SJ, Gerhardt S, Grist M, Hamlin GA, James MJ, Jones EV, Karoutchi GI, Kenny PW, Morley AD, Oldham K,Rankine N, Ryan D, Wells SL, Wood L, Augustin M, Krapp S, Simader H, Steinbacher S.  Dipeptidyl nitrile inhibitors of Cathepsin L. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3.