SML3229
LY3000328
≥95% (HPLC)
别名:
(3R,4S)-4-(4-Fluorobenzamido)-6-(4-(oxetan-3-yl)piperazin-1-yl)chroman-3-yl methylcarbamate, LY 3000328, LY-3000328, N-[(3R,4S)-3,4-Dihydro-3-[[(methylamino)carbonyl]oxy]-6-[4-(3-oxetanyl)-1-piperazinyl]-2H-1-benzopyran-4-yl]-4-fluorobenzamide
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About This Item
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质量水平
方案
≥95% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
O=C(C(C=C1)=CC=C1F)N[C@H]2C3=CC(N4CCN(C5COC5)CC4)=CC=C3OC[C@@H]2OC(NC)=O
InChI
1S/C25H29FN4O5/c1-27-25(32)35-22-15-34-21-7-6-18(29-8-10-30(11-9-29)19-13-33-14-19)12-20(21)23(22)28-24(31)16-2-4-17(26)5-3-16/h2-7,12,19,22-23H,8-11,13-15H2,1H3,(H,27,32)(H,28,31)/t22-,23-/m0/s1
InChI key
NDEBZCZEAVMSQF-GOTSBHOMSA-N
生化/生理作用
LY3000328 is an orally active, non-covalent, potent and selective cathepsin S (Cat S, Cat-S, CatS, CTSS) inhibitor (human/mouse CatS IC50 = 7.7/1.67 nM) that targets the S2 and S3 subsites without interacting with the active site Cys25. LY3000328 prevents high glucose-induced human aortic smooth muscle cells (SMCs) osteogenic transformation in cultures (1 µM) and displays in vivo therapeutic efficacy in murine models of CaCl2-induced abdominal aortic aneurysm (AAA) (1-10 mg/kg bid po) and CD4+ T cell-mediated colitis induction (0.1 mg/0.2 mL/mouse via daily i.p.).
Orally active, non-covalent, potent and selective cathepsin S (Cat S, Cat-S, CatS, CTSS) inhibitor in vitro and in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Christopher D Payne et al.
British journal of clinical pharmacology, 78(6), 1334-1342 (2014-07-22)
The aim of this study was to assess the safety and tolerability, pharmacokinetics and pharmacodynamics of LY3000328 when administered as single escalating doses to healthy volunteers. This was a phase 1, placebo-controlled, dose escalation study with LY3000328 in 21 healthy
Prabhakar K Jadhav et al.
ACS medicinal chemistry letters, 5(10), 1138-1142 (2014-10-15)
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
Xiaobing Yao et al.
Molecular medicine reports, 20(1), 141-150 (2019-05-23)
As a member of the cysteine protease family, cathepsin S (CTSS) serves an important role in diseases such as cancer, arthritis and atherosclerosis. Nevertheless, its role in renal fibrosis is unknown. In the present study, the effects of CTSS on
Santhosh Kumar Vr et al.
Journal of the American Society of Nephrology : JASN, 27(6), 1635-1649 (2015-11-15)
Endothelial dysfunction is a central pathomechanism in diabetes-associated complications. We hypothesized a pathogenic role in this dysfunction of cathepsin S (Cat-S), a cysteine protease that degrades elastic fibers and activates the protease-activated receptor-2 (PAR2) on endothelial cells. We found that
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