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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Matrix Metalloproteinase (MMP)-TP0628103
TP0628103

Chemical Structure : TP0628103

CAS No.: 2865102-08-3

TP0628103 (TP 0628103)

货号: PC-21674Not For Human Use, Lab Use Only.

TP0628103 is a highly potent, selective matrix metalloproteinase-7 (MMP-7) inhibitor with IC50 of 0.17 nM and 4.1 nM for human and mouse MMP-7, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

TP0628103 is a highly potent, selective matrix metalloproteinase-7 (MMP-7) inhibitor with IC50 of 0.17 nM and 4.1 nM for human and mouse MMP-7, respectively.
TP0628103 exhibits 15,000-fold, 4300-fold, and 10,000-fold selectivity for MMP-7 over MMP-2, MMP-12, and MMP-14, respectively.
TP0628103 also displays excellent (>59,000-fold) selectivity against MMP-1, -3, -8, -9, and -13 and low OATP-mediated hepatic uptake ratios (OATP1B1:1.20, OATP1B3:2.08).
TP0628103 (0.3 mg/kg/day) reduced renal collagen and caused significant inhibition of collagen production in mouse model of UUO-induced renal fibrosis.

物理化学性质&存储条件

分子量 1134.67
分子式 C51H67ClF3N11O11S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N5-(2-(((S)-1-(((S)-1-((4-(4-(((R)-6-amino-1-((S)-3-aminopyrrolidin-1-yl)-1-oxohexan-2-yl)carbamoyl)piperidine-1-carbonyl)phenyl)amino)-3,3-dimethyl-1-oxobutan-2-yl)amino)-1-oxo-3-(pyridin-4-yl)propan-2-yl)amino)-2-oxoethyl)-N2-((4-chloro-3-(trifluoromethyl)phenyl)sulfonyl)-L-glutamine

参考文献

1. Yusuke Oka, et al. J Med Chem. 2024 Jan 12. doi: 10.1021/acs.jmedchem.3c01967.

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