A potent EP2 receptor antagonist (Kb = 17.8 nM in C6 glioma cells overexpressing human EP2); 300-

TG6-10-1 – 5 mg

Brand:
Cayman
CAS:
1415716-58-3
Storage:
-20
UN-No:
Non-Hazardous - /

TG6-10-1 is a potent antagonist of E prostanoid receptor 2 (EP2; Kb = 17.8 nM in C6 glioma cells overexpressing human EP2).{40354} It is 300-, 25-, and 10-fold selective for EP2 over other prostanoid receptors, including human EP3-4, FP and TP, and DP1 receptors, respectively. TG6-10-1 is also selective for EP2 over a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s >10 μM). In vivo, TG6-10-1 increases survival, decreases weight loss, prevents induction of IL-1β, IL-6, TNF-α, and MCP-1/CCL2 mRNA, and inhibits neuronal cell death in the hippocampus in mouse and rat models of status epilepticus induced by pilocarpine (Item No. 14487) and diisopropyl fluorophosphate, respectively.{40354,40355}  

 

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SKU: 23444 - 5 mg Category:

Description

A potent EP2 receptor antagonist (Kb = 17.8 nM in C6 glioma cells overexpressing human EP2); 300-, 25-, and 10-fold selective for EP2 over other human EP3-4, FP and TP, and DP1 receptors, respectively; selective for EP2 over a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s >10 μM); increases survival, decreases weight loss, prevents induction of IL-1β, IL-6, TNF-α, and MCP-1/CCL2 mRNA, and inhibits neuronal cell death in the hippocampus in mouse and rat models of status epilepticus induced by pilocarpine and diisopropyl fluorophosphate, respectively

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

Synonyms: 

Molecular weight: 448.4

CAS: 1415716-58-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway||Research Area|Neuroscience|Seizure Disorders

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