5.05765

Prostaglandin EP2 Receptor Antagonist, TG6-10-1

• Synonim(y): Prostaglandin EP2 Receptor Antagonist, TG6-10-1, (E)-N-(2-(2-(trifluoromethyl)-1H-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide, EP2 Antagonist, TG6-10-1
• Wzór empiryczny (zapis Hilla): C₂₃H₂₃F₃N₂O₄
• Numer CAS: 1415716-58-3
• Masa cząsteczkowa: 448.43
• Kod UNSPSC: 12352211
• Identyfikator substancji w PubChem: 71499384
• NACRES: NA.77

Właściwości

• Próba: ≥98% (HPLC)
• Poziom jakości: 100
• Postać: powder
• siła działania: 17.8 nM K_i
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white
• rozpuszczalność: DMSO: 100 mg/mL
• temp. przechowywania: 2-8°C
• ciąg SMILES: COC1=CC(=CC(=C1OC)OC)C=CC(=O)NCCN2C3=CC=CC=C3C=C2C(F)(F)F

Opis

Opis ogólny

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.).

Działania biochem./fizjol.

Primary Target
EP2

Reversible: yes

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable