CFM-2

SKU: orb1710082

Description

CFM-2 is a potent and selective non-competitive AMPA receptor antagonist. It demonstrates robust anticonvulsant efficacy in diverse in vivo seizure models, making it a valuable research tool for studying excitatory neurotransmission and epilepsy pathophysiology.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 178616-26-7
• MW: 311.34
• Purity: 97.16% (May vary between batches)
• Formula: C₁₇H₁₇N₃O₃
• SMILES: COc1cc2CC(=O)NN=C(c3ccc(N)cc3)c2cc1OC
• Target: iGluR
• Solubility: DMSO:45 mg/mL (144.54 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.42 mM)

Bioactivity

• In Vivo:
  Pretreatment with CFM-2 delayed the progression of seizure rank during repeated administration of pentylenetetrazole. At the end of the period of repeated pentylenetetrazole treatment (6 weeks), the mean seizure score was 0 in vehicle-treated controls, 4.3 in animals treated with vehicle + pentylenetetrazole, 2.2 in rats treated chronically with CFM-2 (20 μmol/kg i.p.) + pentylenetetrazole and 1.0 in rats treated repeatedly with CFM-2 (50 μmol/kg i.p.) + pentylenetetrazole. CFM-2 was also able to antagonize the long-term increase in sensitivity of the convulsant effects of GABA function inhibitors in pentylenetetrazole-kindled animals . CFM-2 has been proven to possess anticonvulsant activity in various models of seizures . Intrathecal application of two selective non-competitive AMPAR antagonists, CFM-2 (25 and 50 μg) and GYKI 52466 (50 μg), significantly attenuated mechanical and thermal hypersensitivities on the ipsilateral hind paw at 2 and 24 h post-CFA injection. Neither CFM-2 nor GYKI 52466 affected the contralateral basal responses to thermal and mechanical stimuli .
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• In Vitro:
  CFM-2 inhibits the extracellular signal-regulated kinase (ERK1/2) pathway, reduces phosphorylation of cAMP-responsive element-binding protein (CREB), and suppresses cyclin D1 expression. It upregulates cell cycle regulators and tumor suppressor proteins p21 and p53, consequently decreasing lung adenocarcinoma cell populations in the G2 and S phases of the cell cycle.
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Storage & Handling

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

Alternative Names

CFM 2, CFM2, CFM-2, AMPAR

Compound Identifiers

PubChem CID

4377504