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首页-小分子抑制剂&激动剂-GPCR-Angiotensin Receptor-YK-4-250
YK-4-250

Chemical Structure : YK-4-250

CAS No.: 1276682-49-5

YK-4-250

货号: PC-27777Not For Human Use, Lab Use Only.

YK-4-250 is a Tempol-conjugated angiotensin receptor blocker (TCARB), selectively inhibits Angiotensin II type 1 receptor (AT1R) with IC50 of 1 nM, shows potential for protecting and mitigating radiation-induced injury.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

YK-4-250 is a Tempol-conjugated angiotensin receptor blocker (TCARB), selectively inhibits Angiotensin II type 1 receptor (AT1R) with IC50 of 1 nM, shows potential for protecting and mitigating radiation-induced injury.
YK-4-250 does not inhibit AT2R.
YK-4-250 (50 uM) inhibits cellular ROS following stimulation of ROS production in Caco-2 cells.
YK-4-250 retains the antioxidant properties of tempol and demonstrates increase ACE2 expression.
YK-4-250 (daily oral dose of 20 mg/kg)protects and mitigates radiation damage at LD50 dose of PBI and improves overall survival in male C57BL/6 mice.
YK-4-250 decreases in vivo oxidative stress and increases membrane ACE2 protein levels.
YK-4-250 reduces DNA damage and enhances DNA repair following IR.
YK-4-250 is stable in vivo and can be imaged by EPR and MRI.

物理化学性质&存储条件

分子量 668.85
分子式 C42H46N5O3
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

1-Piperidinyloxy, 4-[[[4′-[(1,4′-dimethyl-2′-propyl[2,6′-bi-1H-benzimidazol]-1′-yl)methyl][1,1′-biphenyl]-2-yl]carbonyl]oxy]-2,2,6,6-tetramethyl-

参考文献

1. Kumar VP, et al. Sci Rep. 2026 May 26;16(1):23964.

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