225120-65-0Cathepsin Inhibitor 1
225120-65-0
产品详情:
- 中文名称:
- Cathepsin Inhibitor 1
- 英文名称:
- Cathepsin Inhibitor 1
- CAS号:
- 225120-65-0
- 品牌:
- 一研
- 保存条件:
- Store at -20°C
- 产品类别:
- 抑制剂
- Cas:
- 225120-65-0
产品属性:
产品名称 | 规格 | CAS号 | 型号 |
Cathepsin Inhibitor 1 | 5mg 100mg | 225120-65-0 | EY-Y0163998 |
Cas No.225120-65-0
别名
化学名 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
储存条件 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
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.
公司简介
成立日期 | (11年) |
注册资本 | 100 |
员工人数 | 50-100人 |
年营业额 | ¥ 100万以内 |
经营模式 | 工厂,试剂 |
主营行业 | 生化试剂,抗体,细胞培养,分子生物学,免疫安全 |
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