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VBY-825
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。
VBY-825图片
CAS NO:1310340-58-9
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议

产品介绍

VBY-825是cathepsin新型可逆抑制剂,对cathepsinB,L,S和V都具有很高的抑制力。

Cas No.1310340-58-9
Canonical SMILESCC[C@H](NC([C@@H](N[C@@H](C1=CC=C(F)C=C1)C(F)(F)F)CS(=O)(CC2CC2)=O)=O)C(C(NC3CC3)=O)=O
分子式C23H29F4N3O5S
分子量535.55
溶解度DMSO : 125 mg/mL (233.40 mM);Water :< 0.1 mg/mL (insoluble)
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

VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.IC50 value: Target: 130/250/250/330/2.3/4.7 nM(Ki for cathepsin S/L/ZV/Bhumanized-rabbit cathepsin K/cathepsin F) [1]VBY-825 is a potent inhibitor of the assayed cathepsins and its potency against at least one cathepsin, cathepsin S, extends across species relevant for pharmacology studies, specifically mouse. 10 mg/kg/day dose of VBY-825 achieves a trough plasma concentration >200nM, which is well above that required for full inhibition of the intracellular activity of cathepsins B, F, K, L, S and V in both mouse and human cell lines.

[1]. Elie BT, et al. Identification and pre-clinical testing of a reversible cathepsin protease inhibitor reveals anti-tumor efficacy in a pancreatic cancer model. Biochimie. 2010 Nov;92(11):1618-24.