A selective

TG4-155 – 10 mg

Brand:
Cayman
CAS:
1164462-05-8
Storage:
-20
UN-No:
Non-Hazardous - /

Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection.{11615,23324,26528} TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels.{28703,28704} It blocks the induced expression of inflammatory markers in microglial cells treated with the selective EP2 agonist butaprost (Item No. 13740) alone or with LPS and IFNγ.{28703,23348} TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine (Item No. 14487).{28703} It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost.{28704}  

 

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Description

A selective, brain penetrant EP2 antagonist (KB = 2.4 nM); blocks the induced expression of inflammatory markers in microglial cells treated with butaprost; reduces neurodegeneration in a mouse model of status epilepticus; inhibits proliferation and invasion in cancer cells treated with butaprost

Formal name: (2E)-N-[2-(2-methyl-1H-indol-1-yl)ethyl]-3-(3,4,5-trimethoxyphenyl)-2-propenamide

Synonyms: 

Molecular weight: 394.5

CAS: 1164462-05-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway||Research Area|Neuroscience|Neurodegenerative Disorders||Research Area|Neuroscience|Seizure Disorders

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