TG 4-155

SKU: orb1301754

Description

TG4-155 is a potent and selective brain-penetrant antagonist of the EP2 receptor (K_B = 2.4 nM), exhibiting >1000-fold selectivity over EP4 and other off-targets. This profile makes it a valuable research tool for investigating EP2-mediated neuroinflammation, neurodegeneration, and pain in both cellular and animal models.

Research Area

Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1164462-05-8
• MW: 394.47
• Purity: >98%
• Formula: C₂₃H₂₆N₂O₄
• SMILES: COc1cc(\C=C\C(=O)NCCn2c(C)cc3ccccc23)cc(OC)c1OC
• Target: GPCR
• Solubility: Soluble in DMSO (up to 35 mg/ml) or in Ethanol (up to 10 mg/ml).

Bioactivity

• Target IC50:
  EP2 receptor:9.9 nM (Ki)
• 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.
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• 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.
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• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, EP2, inhibit, TG4 155, TG4155, TG-4-155, TG4-155, Prostaglandin Receptor, ProstaglandinReceptor

Compound Identifiers

PubChem CID

5886965