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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-ROCK-TDI01
TDI01

Chemical Structure : TDI01

CAS No.: 2260506-59-8

TDI01 (TDI-01, TDI-01470, TDI01470)

货号: PC-26805Not For Human Use, Lab Use Only.

TDI01 (TDI01470) is a potent, highly selective Rho-associated coiled-coil containing kinase 2 (ROCK2) inhibitor with IC50 of 10.31 nM, 598-fold selectivity over ROCK1.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TDI01 (TDI01470) is a potent, highly selective Rho-associated coiled-coil containing kinase 2 (ROCK2) inhibitor with IC50 of 10.31 nM, 598-fold selectivity over ROCK1.
TDI01 exhibits high-affinity binding to ROCK2 (KD=65.56 nM) in BLI assays, with negligible binding to ROCK1 up to 60 uM.
TDI01 exhibits dose-dependent inhibition of ROCK2 activity in ECs and LX2 cells.
TDI01 (5 mg/kg, oral) decreased serum ALT and AST levels, lowered hepatic HYP content, alleviated liver collagen deposition, and reduced steatosis in mouse MASH model.
TDI01 is at least partially mediated by attenuating the production of pro-fibrotic galectin-3 from liver ECs.

物理化学性质&存储条件

分子量 485.50
分子式 C26H21F2N7O
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

(6-(4-((4-(1H-pyrazol-4-yl)phenyl)amino)pyrimidin-2-yl)-1-methyl-1H-indol-2-yl)(3,3-difluoroazetidin-1-yl)methanone

参考文献

1. Hu Y, et al. Cell. 2026 Apr 30;189(9):2663-2683.e26.

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