TG6-10-1

TG6-10-1 is a potent and selective antagonist for the prostaglandin E2 receptor subtype EP2. Systemic administration of TG6-10-1 completely recapitulates the effects of conditional ablation of cyclooxygenase-2 from principal forebrain neurons, namely reduced delayed mortality, accelerated recovery from weight loss, reduced brain inflammation, prevention of blood-brain barrier opening, and neuroprotection in the hippocampus, without modifying seizures acutely. TG6-10-1 shows low-nanomolar antagonist activity against EP2.

Product information

CAS Number: 1415716-58-3

Molecular Weight: 448.43

Formula: C23H23F3N2O4

Synonym:

TP-6101

TG6-10-1

TG 6-10-1

TG-6-10-1

TP6101

TP 6101

Chemical Name: (E)-N-(2-(2-(trifluoromethyl)-1H-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide

Smiles: COC1C(=CC(=CC=1OC)/C=C/C(=O)NCCN1C2=CC=CC=C2C=C1C(F)(F)F)OC

InChiKey: WUYOECAJFJFUFC-CMDGGOBGSA-N

InChi: 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)/b9-8+

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

TG6-10-1 robustly blocks prostaglandin E2 (PGE2) (10 μM)-induced cAMP accumulation in a concentration-dependent manner in SH-SY5Y cells.

In Vivo:

TG6-10-1 (5 mg/kg; i.p.; 4-30 hours) improves survival, accelerates recovery of lost weight, and improves functional recovery following status epilepticus (SE) .

References:

1. Rojas A, Ganesh T, Lelutiu N, Gueorguieva P, Dingledine R. Inhibition of the prostaglandin EP2 receptor is neuroprotective and accelerates functional recovery in a rat model of organophosphorus induced status epilepticus. Neuropharmacology. 2015 Jun;93:15-27. doi:10.1016/j.neuropharm.2015.01.017. Epub 2015 Feb 3. PubMed PMID: 25656476; PubMed Central PMCID: PMC4387070.
2. Jiang J, Quan Y, Ganesh T, Pouliot WA, Dudek FE, Dingledine R. Inhibition of the prostaglandin receptor EP2 following status epilepticus reduces delayed mortality and brain inflammation. Proc Natl Acad Sci U S A. 2013 Feb 26;110(9):3591-6. doi: 10.1073/pnas.1218498110. Epub 2013 Feb 11. PubMed PMID:23401547; PubMed Central PMCID: PMC3587237.

Products are for research use only. Not for human use.