產(chǎn)品屬性:
產(chǎn)品名稱 | 規(guī)格 | CAS號 | 型號 |
Cathepsin G Inhibitor I | 500ug 1mg 5mg | 429676-93-7 | EY-Y0163999 |
Cas No.429676-93-7
別名 N/A
化學(xué)名 [2-[3-[(1-benzoylpiperidin-4-yl)-methylcarbamoyl]naphthalen-2-yl]-1-naphthalen-1-yl-2-oxoethyl]phosphonic acid
分子式 C36H33N2O6P
分子量 620.64
溶解度 ≥ 10.35mg/mL 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(chǎn)品描述:
IC50: 53 nM
Cathepsin G (EC 3.4.21.20, chymotrypsin-like proteinase, neutral proteinase) is an enzymatic protein belonging to the peptidase or protease families. In humans, it is coded by the CTSG gene. Cathepsin G Inhibitor I is a potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G.
In vitro: Cathepsin G Inhibitor I shows reversible, competitive inhibition with IC50 and Ki values of 53 ± 12 (N = 10) and 63 ± 14 nM (N = 5), respectively. Another attribute of Cathepsin G Inhibitor I relates to its selectivity vs other serine proteases. It weakly inhibits chymotrypsin (Ki = 1.5 ± 0.2 μM), and poorly inhibits (<50% inhibition at 100 μM) thrombin, factor Xa, factor IXa, plasmin, trypsin, tryptase, proteinase 3, and human leukocyte elastase [1].
In vivo: Cathepsin G Inhibitor I is currently in in-vitro investigation and no animal in vivo study is ongoing [1].
Clinical trial: Cathepsin G Inhibitor I is currently in the preclinical development and no clinical trial is ongoing.
Reference:
[1] Greco MN, Hawkins MJ, Powell ET, Almond HR Jr, Corcoran TW, de Garavilla L, Kauffman JA, Recacha R, Chattopadhyay D, Andrade-Gordon P, Maryanoff BE. Nonpeptide inhibitors of cathepsin G: optimization of a novel beta-ketophosphonic acid lead by structure-based drug design. J Am Chem Soc. 2002;124(15):3810-1.
關(guān)鍵字: 429676-93-7;C36H33N2O6P;Cathepsin G Inhibito;
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