TG11-77 | PEG2 receptor inhibitor | Probechem Biochemicals

Chemical Structure : TG11-77

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TG11-77 (TG11-77 HCl)

货号: PC-49574Not For Human Use, Lab Use Only.

TG11-77 is a potent, selective, brain-permeable and orally available antagonist of the prostaglandin E2 (PGE2) receptor subtype EP2 with KB value of 9.7 nM.

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生物&药学活性

TG11-77 is a potent, selective, brain-permeable and orally available antagonist of the prostaglandin E2 (PGE2) receptor subtype EP2 with KB value of 9.7 nM.
TG11-77 is selective for EP2 over DP1, EP4, and IP receptors (KBs=7,320, 5,300, and >10,000 nM, respectively).
TG11-77 inhibits the expression of genes encoding COX-2, IL-1β, and IL-6 induced by LPS and the EP2 receptor agonist ONO-AE1-259-01 in mouse BV-2 microglia expressing human EP2 receptors.
TG11-77 eliminates the profound cognitive deficit in Y-maze performance after SE and reduces delayed mortality and microgliosis, with a minimum effective i.p. dose (as free base) of 8.8 mg/kg.

物理化学性质&存储条件

分子量	436.944
分子式	C23H25ClN6O
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	2-((4,6-dimethylpyridin-2-yl)amino)-N-(2-(2-methyl-1H-indol-3-yl)ethyl)pyrimidine-5-carboxamide, monohydrochloride

参考文献

1. Radhika Amaradhi, et al. J Med Chem. 2020 Feb 13;63(3):1032-1050.

2. Nicholas H Varvel , et al. Neuropharmacology. 2022 Nov 30;224:109356.

TG11-77 (TG11-77 HCl)

生物&药学活性

物理化学性质&存储条件

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TG11-77 (TG11-77 HCl)

生物&药学活性

物理化学性质&存储条件

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