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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Discoidin Domain Receptor (DDR)-CH6824025
CH6824025

Chemical Structure : CH6824025

CAS No.: 1476756-15-6

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CH6824025 (CH 6824025)

货号: PC-23135Not For Human Use, Lab Use Only.

CH6824025 is a potent, selective discoidin domain receptor 1 (DDR1) inhibitor, dose-dependently inhibits the phosphorylation of DDR1 induced by adding Type 1 collagen to U2OS cells stably expressing DDR1 with IC50 of 8.9 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CH6824025 is a potent, selective discoidin domain receptor 1 (DDR1) inhibitor, dose-dependently inhibits the phosphorylation of DDR1 induced by adding Type 1 collagen to U2OS cells stably expressing DDR1 with IC50 of 8.9 nM.
CH6824025 is highly selective, because the 451 types of kinases evaluated by KINOMEscan, only
DDR1, DDR2, and Lymphocyte-Oriented Kinase (LOK) showed more than 99% competitive
binding inhibition at 1 uM.
CH6824025 suppresses the phosphorylation of DDR1 in the kidney, and the amount of hydroxyproline, the Sirius red- and the F4/80-positive area.
CH6824025 significantly decreases the mRNA expression of fibrosis and inflammation-related genes in the kidney were significantly decreased.
CH6824025 could ameliorate fibrosis and inflammation in unilateral ureteral obstruction (UUO) mice.
CH6824025 inhibits cell motility (e.g., migration) that prevents the progression of fibrosis and improves mitochondrial function in UUO mice.

物理化学性质&存储条件

分子量 566.46
分子式 C24H28Cl2F3N3O3S
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

3-chloro-N-[(5-chloro-2-ethylsulfonylphenyl)methyl]-4-[[(3S)-3-(methylamino)piperidin-1-yl]methyl]-5-(trifluoromethyl)benzamide

参考文献

1. Yasui Y, et al. J Pharmacol Exp Ther. 2024 Oct 8:JPET-AR-2024-002330.

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