TG6-10-1


Catalog No. size PriceQuantity
M6610-2 2mg solid $141
M6610-10 10mg solid $553

Description

Cas:1415716-58-3

Product Information

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.

 

Chemical Formula: C23H23F3N2O4

 

Exact Mass: 448.16099

 

Molecular Weight: 448.44

 

Elemental Analysis: C, 61.60; H, 5.17; F, 12.71; N, 6.25; O, 14.27

 

Synonym: 

 

TG6-10-1

TG 6-10-1

TG-6-10-1

TP6101

TP-6101

TP 6101

 

Chemical Name:

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

 

InChi Key:

WUYOECAJFJFUFC-CMDGGOBGSA-N

 

InChi Code: 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+

 

Smiles Code:

O=C(NCCN1C(C(F)(F)F)=CC2=C1C=CC=C2)/C=C/C3=CC(OC)=C(OC)C(OC)=C3

 

 

Technical Data:

 

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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.

 

  1. 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.

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