TG6-10-1 | CAS#1415716-58-3 | EP2 antagonist

MedKoo Cat#: 522512 | Name: TG6-10-1

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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 Structure

TG6-10-1

CAS#1415716-58-3

Theoretical Analysis

MedKoo Cat#: 522512

Name: TG6-10-1

CAS#: 1415716-58-3

Chemical Formula: C23H23F3N2O4

Exact Mass: 448.1610

Molecular Weight: 448.44

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

Price and Availability

Size	Price	Availability
5mg	USD 150.00	Ready to Ship
10mg	USD 250.00	Ready to ship
25mg	USD 450.00	Ready to ship
50mg	USD 750.00	Ready to ship
100mg	USD 1,250.00	Ready to ship
200mg	USD 2,050.00	Ready to ship

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Related CAS #

No Data

Synonym

TG6-10-1; TG 6-10-1; TG-6-10-1; TP6101; TP-6101; TP 6101.

IUPAC/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

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

More Info

Certificate of Analysis

View CoA: current batch, Lot#CRB60415

QC Data

View QC data: current batch, Lot# CRB60415

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 448.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Rawat V, Banik A, Amaradhi R, Rojas A, Taval S, Nagy T, Dingledine R, Ganesh T. Pharmacological antagonism of EP2 receptor does not modify basal cardiovascular and respiratory function, blood cell counts, and bone morphology in animal models. Biomed Pharmacother. 2022 Mar;147:112646. doi: 10.1016/j.biopha.2022.112646. Epub 2022 Jan 26. PMID: 35091236; PMCID: PMC8854338. 2: Brennan GP, Garcia-Curran MM, Patterson KP, Luo R, Baram TZ. Multiple Disruptions of Glial-Neuronal Networks in Epileptogenesis That Follows Prolonged Febrile Seizures. Front Neurol. 2021 Feb 18;12:615802. doi: 10.3389/fneur.2021.615802. PMID: 33679583; PMCID: PMC7930821. 3: Yu Y, Jiang J. COX-2/PGE2 axis regulates hippocampal BDNF/TrkB signaling via EP2 receptor after prolonged seizures. Epilepsia Open. 2020 Jun 9;5(3):418-431. doi: 10.1002/epi4.12409. PMID: 32913950; PMCID: PMC7469770. 4: Jiang C, Caskurlu A, Ganesh T, Dingledine R. Inhibition of the prostaglandin EP2 receptor prevents long-term cognitive impairment in a model of systemic inflammation. Brain Behav Immun Health. 2020 Aug 25;8:100132. doi: 10.1016/j.bbih.2020.100132. PMID: 34589882; PMCID: PMC8474496. 5: Li L, Yu Y, Hou R, Hao J, Jiang J. Inhibiting the PGE2 Receptor EP2 Mitigates Excitotoxicity and Ischemic Injury. ACS Pharmacol Transl Sci. 2020 Jun 25;3(4):635-643. doi: 10.1021/acsptsci.0c00040. PMID: 32832866; PMCID: PMC7432651. 6: Amaradhi R, Banik A, Mohammed S, Patro V, Rojas A, Wang W, Motati DR, Dingledine R, Ganesh T. Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist for Use in Central Nervous System Disease Models. J Med Chem. 2020 Feb 13;63(3):1032-1050. doi: 10.1021/acs.jmedchem.9b01218. Epub 2020 Jan 16. PMID: 31904232; PMCID: PMC7394479. 7: Rojas A, Ganesh T, Wang W, Wang J, Dingledine R. A rat model of organophosphate-induced status epilepticus and the beneficial effects of EP2 receptor inhibition. Neurobiol Dis. 2020 Jan;133:104399. doi: 10.1016/j.nbd.2019.02.010. Epub 2019 Feb 25. PMID: 30818067; PMCID: PMC6708729. 8: Jiang J, Yu Y, Kinjo ER, Du Y, Nguyen HP, Dingledine R. Suppressing pro- inflammatory prostaglandin signaling attenuates excitotoxicity-associated neuronal inflammation and injury. Neuropharmacology. 2019 May 1;149:149-160. doi: 10.1016/j.neuropharm.2019.02.011. Epub 2019 Feb 11. PMID: 30763657; PMCID: PMC6486887. 9: Qiu J, Li Q, Bell KA, Yao X, Du Y, Zhang E, Yu JJ, Yu Y, Shi Z, Jiang J. Small-molecule inhibition of prostaglandin E receptor 2 impairs cyclooxygenase- associated malignant glioma growth. Br J Pharmacol. 2019 Jun;176(11):1680-1699. doi: 10.1111/bph.14622. Epub 2019 Apr 29. PMID: 30761522; PMCID: PMC6514294. 10: Lin X, Liu X, Guo C, Liu M, Mi Y, Zhang C. Promotion of the prehierarchical follicle growth by postovulatory follicles involving PGE2 -EP2 signaling in chickens. J Cell Physiol. 2018 Nov;233(11):8984-8995. doi: 10.1002/jcp.26844. Epub 2018 Jun 19. PMID: 29923198. 11: Kang X, Qiu J, Li Q, Bell KA, Du Y, Jung DW, Lee JY, Hao J, Jiang J. Cyclooxygenase-2 contributes to oxidopamine-mediated neuronal inflammation and injury via the prostaglandin E2 receptor EP2 subtype. Sci Rep. 2017 Aug 25;7(1):9459. doi: 10.1038/s41598-017-09528-z. PMID: 28842681; PMCID: PMC5573328. 12: Greaves E, Horne AW, Jerina H, Mikolajczak M, Hilferty L, Mitchell R, Fleetwood-Walker SM, Saunders PT. EP2 receptor antagonism reduces peripheral and central hyperalgesia in a preclinical mouse model of endometriosis. Sci Rep. 2017 Mar 10;7:44169. doi: 10.1038/srep44169. PMID: 28281561; PMCID: PMC5345039. 13: Rojas A, Ganesh T, Manji Z, O'neill T, Dingledine R. Inhibition of the prostaglandin E2 receptor EP2 prevents status epilepticus-induced deficits in the novel object recognition task in rats. Neuropharmacology. 2016 Nov;110(Pt A):419-430. doi: 10.1016/j.neuropharm.2016.07.028. Epub 2016 Jul 29. PMID: 27477533; PMCID: PMC5028311. 14: Hayashi Y, Morinaga S, Liu X, Zhang J, Wu Z, Yokoyama T, Nakanishi H. An EP2 Agonist Facilitates NMDA-Induced Outward Currents and Inhibits Dendritic Beading through Activation of BK Channels in Mouse Cortical Neurons. Mediators Inflamm. 2016;2016:5079597. doi: 10.1155/2016/5079597. Epub 2016 May 19. PMID: 27298516; PMCID: PMC4889853. 15: 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. PMID: 25656476; PMCID: PMC4387070. 16: Jiang J, Yang MS, Quan Y, Gueorguieva P, Ganesh T, Dingledine R. Therapeutic window for cyclooxygenase-2 related anti-inflammatory therapy after status epilepticus. Neurobiol Dis. 2015 Apr;76:126-136. doi: 10.1016/j.nbd.2014.12.032. Epub 2015 Jan 17. PMID: 25600211; PMCID: PMC4408774. 17: 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. PMID: 23401547; PMCID: PMC3587237.