13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
聯系人:高小姐
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Q Q： 3004967995
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詳細地址：上海嘉定區嘉羅公路1661
| 規格 | 5mg 100mg |
| CAS | 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 |
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.
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原創作者：上海莼試生物技術有限公司
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賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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