產品屬性：
產品名稱 | 規(guī)格 | CAS號 | 型號 |
Cathepsin Inhibitor 1 | 5mg 100mg | 225120-65-0 | EY-Y0163998 |
Cas No.225120-65-0
別名
化學名 5-tert-butyl-N-[(2S)-3-(3-chlorophenyl)-1-(cyanomethylamino)-1-oxopropan-2-yl]-2-methylpyrazole-3-carboxamide
分子式 C20H24ClN5O2
分子量 401.89
溶解度 Soluble in DMSO
儲存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
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.
關鍵字： 225120-65-0;C20H24ClN5O2;Cathepsin Inhibitor ;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學、分子生物學和常規(guī)生化試劑等為一體的科研產品銷售企業(yè)，公司自成立以來，秉承""全心全意服務于科研工作者""的企業(yè)理念，立足生物科技領域，運用生物技術和科研試劑，發(fā)展現代生物科技，為各類大中小醫(yī)院及其它醫(yī)療機構、高等院校、科研院所、企事業(yè)單位提供優(yōu)質的產品，服務生物科技領域的科學研究人員。
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