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TG4-155

Catalog No. T5482   CAS 1164462-05-8

TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 μM) and a panel of other receptors and channels

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TG4-155 Chemical Structure
TG4-155, CAS 1164462-05-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 30.00
2 mg In stock $ 44.00
5 mg In stock $ 68.00
10 mg In stock $ 109.00
25 mg In stock $ 231.00
50 mg In stock $ 401.00
100 mg In stock $ 597.00
1 mL * 10 mM (in DMSO) In stock $ 75.00
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Purity: 99.14%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 μM) and a panel of other receptors and channels
Targets&IC50 EP2 Receptor:9.9 nM (Ki)
In vitro TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 μM) and a panel of other receptors and channels[1].
In vivo TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine. It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost[2].
Cell Research Cytotoxicity of TG4-155 was examined with the CellTiter-Glo Luminescent Cell Viability Assay by measuring cellular ATP level, which correlates with cell viability.?Briefly, C6G cells were plated in 384-well plates at 2,000 cells/well in 25 μl DMEM plus test compound and incubated for 2 days.?CellTiter-Glo reagent (25 μl) was then added to each well.?The contents were mixed for 2 minutes on an orbital shaker to induce cell lysis and incubated at room temperature for 10 minutes.?Relative viability is proportional to luminescence intensity as measured by a microplate reader with an integration time of 1 second[2].
Animal Research C57BL/6 mice (8 12 wk old) were injected with pilocarpine (280 mg/kg, i.p.) to induce status epilepticus (SE). SE was allowed for 1 h and terminated by pentobarbital (30 mg/kg, i.p.). Mice were then randomized by assignment to a random number stream and received two doses of vehicle or TG4-155 (5 mg/kg, i.p.) at 1 and 12 h after SE termination. Mice were euthanized under deep isoflurane anesthesia 24 h after SE and brains were collected for histology[1].
Molecular Weight 394.46
Formula C23H26N2O4
CAS No. 1164462-05-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (316.89 mM)

TargetMolReferences and Literature

1. Jiang J , Ganesh T , Du Y , et al. Small molecule antagonist reveals seizure-induced mediation of neuronal injury by prostaglandin E2 receptor subtype EP2[J]. Proceedings of the National Academy of Sciences, 2012, 109(8):3149-3154. 2. Jiang J , Dingledine R . Role of Prostaglandin Receptor EP2 in the Regulations of Cancer Cell Proliferation, Invasion, and Inflammation[J]. Journal of Pharmacology and Experimental Therapeutics, 2012, 344(2):360-367.

Related compound libraries

This product is contained In the following compound libraries:
Immunology/Inflammation Compound Library Covalent Inhibitor Library CNS-Penetrant Compound Library Anti-Cancer Compound Library Endocrinology-Hormone Compound Library Bioactive Compounds Library Max Anti-Aging Compound Library Inhibitor Library NO PAINS Compound Library GPCR Compound Library

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Keywords

TG4-155 1164462-05-8 GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor inhibit TG-4-155 TG4155 TG4 155 Inhibitor inhibitor

 

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