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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
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 28 € | In Stock | |
2 mg | 41 € | In Stock | |
5 mg | 64 € | In Stock | |
10 mg | 103 € | In Stock | |
25 mg | 219 € | In Stock | |
50 mg | 380 € | In Stock | |
100 mg | 567 € | In Stock | |
1 mL x 10 mM (in DMSO) | 71 € | In Stock |
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 |
Smiles | COc1cc(\C=C\C(=O)NCCn2c(C)cc3ccccc23)cc(OC)c1OC |
Relative Density. | 1.14 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 125 mg/mL (316.89 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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