1373215-15-6 Usage
Description
Z-FL-COCHO, also known as LY3000328, is a potent cathepsin S inhibitor with a high degree of selectivity for cathepsin S over other cathepsin isoforms. It is characterized by its ability to inhibit cathepsin S with an IC50 of 7.7 nM for the human enzyme, while showing significantly lower affinity for cathepsin L, K, B, and V. This selective inhibition makes Z-FL-COCHO a promising compound for various therapeutic applications.
Uses
Used in Pharmaceutical Industry:
Z-FL-COCHO is used as a therapeutic agent for the treatment of abdominal aortic aneurysm. It has demonstrated the ability to reduce aortic diameter in a mouse model of calcium chloride-induced abdominal aortic aneurysm when administered at doses ranging from 1-30 mg/kg.
Additionally, Z-FL-COCHO is used as a potential treatment for plaque instability, atherosclerosis, and autoimmune disorders such as rheumatoid arthritis, psoriasis, and lupus. The compound's mechanism of action involves the inhibition of cathepsin S, which is believed to play a role in the pathogenesis of these conditions. By administering a therapeutically effective amount of Z-FL-COCHO, it may help alleviate the symptoms and progression of these diseases.
references
[1] wiener jj, sun s, thurmond rl. recent advances in the design of cathepsin s inhibitors. curr top med chem. 2010;10(7):717-32.[2] lee-dutra a, wiener dk, sun s. cathepsin s inhibitors: 2004-2010. expert opin ther pat. 2011;21(3):311-37.
Check Digit Verification of cas no
The CAS Registry Mumber 1373215-15-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,7,3,2,1 and 5 respectively; the second part has 2 digits, 1 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 1373215-15:
(9*1)+(8*3)+(7*7)+(6*3)+(5*2)+(4*1)+(3*5)+(2*1)+(1*5)=136
136 % 10 = 6
So 1373215-15-6 is a valid CAS Registry Number.
1373215-15-6Relevant articles and documents
Discovery of cathepsin S inhibitor LY3000328 for the treatment of abdominal aortic aneurysm
Jadhav, Prabhakar K.,Schiffler, Matthew A.,Gavardinas, Kostas,Kim, Euibong J.,Matthews, Donald P.,Staszak, Michael A.,Coffey, D. Scott,Shaw, Bruce W.,Cassidy, Kenneth C.,Brier, Richard A.,Zhang, Yuke,Christie, Robert M.,Matter, William F.,Qing, Keyun,Durbin, Jim D.,Wang, Yong,Deng, Gary G.
, p. 1138 - 1142 (2014/12/10)
Cathepsin S (Cat S) plays an important role in many pathological conditions, including abdominal aortic aneurysm (AAA). Inhibition of Cat S may provide a new treatment for AAA. To date, several classes of Cat S inhibitors have been reported, many of which form covalent interactions with the active site Cys25. Herein, we report the discovery of a novel series of noncovalent inhibitors of Cat S through a medium-throughput focused cassette screen and the optimization of the resulting hits. Structure-based optimization efforts led to Cat S inhibitors such as 5 and 9 with greatly improved potency and drug disposition properties. This series of compounds binds to the S2 and S3 subsites without interacting with the active site Cys25. On the basis of in vitro potency, selectivity, and efficacy in a CaCl2-induced AAA in vivo model, 5 (LY3000328) was selected for clinical development.
