PROSTAGLANDIN EP2 RECEPTOR ANTAGONIST TG6-10-1 (C15-1304-351)

General description

A cell-permeable, 3-acryl-acrylamide derivative that acts as a highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, K_b = 17.8 nM). Exhibits about 300-fold selectivity for the EP2 receptor over human EP3, EP4, and IP receptors, about 100- fold selectivity over human EP1, 25-fold selectivity against human FP and TP, and 10-fold selectivity against human DP1 receptors. Does not affect the activity of about 40 enzymes, ion channels, receptors, and neurotransmitters even at higher concentrations (˜10 µM). Shown to significantly reduce the induction of several inflammatory cytokines and chemokines and reduces the opening of blood-brain barrier during neuronal inflammation. Displays good pharmacokinetic properties with a half-life of 1.6 h and brain to plasma ratio of 1.6 in a murine model (5 mg/kg i.p.).

Biochem/physiol Actions

Primary Target
EP2

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

J. Jiang et al. 2013, PNAS110, 3591.
Jiang. J et al. 2013, PNAS109, 3149.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 448.43. Empirical Formula: C₂₃H₂₃F₃N₂O₄. Assay: ≥. 98% (HPLC). Quality Level: 100. form: powder. potency: 17.8 . nM K_i. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: white. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. SMILES string: COC1: CC(: CC(: C1OC)OC)C: CC(: O)NCCN2C3: CC: CC: C3C: C2C(F)(F)F. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.