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5.05765

Prostaglandin EP2 Receptor Antagonist, TG6-10-1

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C23H23F3N2O4
CAS Number:
1415716-58-3
Molecular Weight:
448.43
UNSPSC Code:
12352211
NACRES:
NA.77
PubChem Substance ID:
71499384
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
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assay

≥98% (HPLC)

Quality Segment

100

form

powder

potency

17.8 nM Ki

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

InChI

1S/C23H23F3N2O4/c1-30-18-12-15(13-19(31-2)22(18)32-3)8-9-21(29)27-10-11-28-17-7-5-4-6-16(17)14-20(28)23(24,25)26/h4-9,12-14H,10-11H2,1-3H3,(H,27,29)

InChI key

WUYOECAJFJFUFC-UHFFFAOYSA-N

General description

A cell-permeable, 3-acryl-acrylamide derivative that acts as a highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, Kb = 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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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