TCN238

SKU: orb1299771

Description

TCN238 is a small molecule, orally bioavailable positive allosteric modulator of mGluR4, exhibiting an EC50 of 1 μM. This research compound is utilized in vitro and in vivo to investigate mGluR4's role in neurological disorders such as Parkinson's disease.

Research Area

Neuroscience

Key Properties

• CAS Number: 125404-04-8
• MW: 197.24
• Purity: 99.90% (May vary between batches)
• Formula: C₁₂H₁₁N₃
• SMILES: Nc1nccc(\C=C\c2ccccc2)n1
• Target: GluR
• Solubility: DMSO:150 mg/mL (760.49 mM);10% DMSO+90% Corn Oil:5 mg/mL (25.35 mM)

Bioactivity

• Target IC50:
  mGluR4:1 μM (EC50)
• In Vivo:
  TCN238 has no activity at the adenosine A2A, serotonin 5-HT1A, or α2A-adrenergic receptors at concentrations up to 10 μM. In a haloperidol-induced catalepsy rat model of Parkinson's disease, it dose-dependently reduces catalepsy with an ED50 of approximately 1 mg/kg. TCN 238 administration in rats leads to downregulation of the mGluR4 gene, GRM4, in the hippocampus and the gene for the GABAA receptor α subunit, GABRA1, in the frontal cortex without affecting hippocampal-dependent memory.
• In Vitro:
  TCN238 has a greater than 30-fold selectivity for mGluR4 over mGluR5 using human recombinant receptors in CHO-K1 cells.

Storage & Handling

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

Alternative Names

TCN238, TCN 238, TCN-238, mGluR, Metabotropic glutamate receptors, inhibit, Inhibitor

Compound Identifiers

PubChem CID

46911068