TG8-260

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].

Product Specifications

CAS Number

[2490544-50-6]

UNSPSC

12352005

Target

Prostaglandin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/tg8-260.html

Purity

99.13

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=C(C2=CN=CN2)C=C1)NCCC3=C(C)NC4=C3C=CC=C4

Molecular Formula

C21H20N4O

Molecular Weight

344.41

References & Citations

[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.