TG6-129 – 5 mg

Brand:
Cayman
CAS:
1164464-14-5
Storage:
-20
UN-No:
Non-Hazardous - /

Prostaglandin E2 (PGE2; Item No. 14010) 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} TG6-129 is an antagonist of the EP2 receptor, suppressing PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 µM.{30786} It is without effect on EP4, DP1, IP, and β2-adrenergic receptors. TG6-129 reduces the expression of COX-2, IL-1β, IL-12, IL-23, IL-6, and TNF-α induced by the EP2-selective agonist butaprost (Item No. 13740) in P388D1 macrophages.{30786} It has low cell cytotoxicity (CC50 = 326 µM), prolonged plasma half-life, and does not cross the blood-brain barrier.{30786}  

 

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Description

A selective antagonist of the EP2 receptor, suppressing PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 µM; reduces the expression of COX-2, IL-1β, IL-12, IL-23, IL-6, and TNF-α induced by the EP2-selective agonist butaprost in P388D1 macrophages


Formal name: (2E)​-N-​[[[4-​[[(5-​ethyl-​1,​3,​4-​thiadiazol-​2-​yl)​amino]​sulfonyl]​phenyl]​amino]​thioxomethyl]​-​3-​(4-​fluorophenyl)​-2-​propenamide

Synonyms:  SID 17503974

Molecular weight: 491.6

CAS: 1164464-14-5

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway