Benzamide, 4-(1H-imidazol-5-yl)-N-[2-(2-methyl-1H-indol-3-yl)ethyl]- Chemical Properties

Boiling point:

718.8±60.0 °C(Predicted)

Density 

1.263±0.06 g/cm3(Predicted)

pka

12.77±0.10(Predicted)

form 

Solid

color 

Off-white to light yellow

Benzamide, 4-(1H-imidazol-5-yl)-N-[2-(2-methyl-1H-indol-3-yl)ethyl]- Usage And Synthesis

Uses

TG8-260 is a second-generation EP2 antagonist developed to alleviate the pathology of central nervous system and peripheral diseases driven by inflammation. TG8-260 can reduce neuroinflammation and gliosis in the hippocampus of rats after pilocarpine-induced persistent epileptic status. Pharmacokinetic data of TG8-260 showed that its plasma half-life was 2.14 hours and its oral bioavailability was 77.3%. TG8-260 is also a potent inhibitor of CYP450 and shows antagonistic activity in inhibiting EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglia, which is suitable for studying anti-inflammatory pathways in animal models of peripheral inflammatory diseases[1].

References

[1] Amaradhi R, Mohammed S, Banik A, et al. Second-generation prostaglandin receptor EP2 antagonist, TG8-260, with high potency, selectivity, oral bioavailability, and anti-inflammatory properties[J]. ACS Pharmacology & Translational Science, 2022, 5(2): 118-133.

Benzamide, 4-(1H-imidazol-5-yl)-N-[2-(2-methyl-1H-indol-3-yl)ethyl]-(2490544-50-6)Related Product Information

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