5.05765

Prostaglandin EP2 Receptor Antagonist, TG6-10-1

• 동의어(들): 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
• 실험식(Hill 표기법): C₂₃H₂₃F₃N₂O₄
• CAS Number: 1415716-58-3
• Molecular Weight: 448.43
• UNSPSC 코드: 12352211
• PubChem Substance ID: 71499384
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• Quality Level: 100
• 형태: powder
• 효능: 17.8 nM K_i
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: white
• solubility: DMSO: 100 mg/mL
• 저장 온도: 2-8°C
• SMILES string: COC1=CC(=CC(=C1OC)OC)C=CC(=O)NCCN2C3=CC=CC=C3C=C2C(F)(F)F

설명

일반 설명

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.).

생화학적/생리학적 작용

Primary Target
EP2

Reversible: yes

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable