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CFM-2

Catalog No. T10774   CAS 178616-26-7

CFM-2 is a selective non-competitive AMPAR antagonist.

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CFM-2 Chemical Structure
CFM-2, CAS 178616-26-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 39.00
5 mg In stock $ 90.00
10 mg In stock $ 136.00
25 mg In stock $ 260.00
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1 mL * 10 mM (in DMSO) In stock $ 100.00
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Purity: 97.16%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CFM-2 is a selective non-competitive AMPAR antagonist.
In vitro CFM-2 inhibits the extracellular signal-regulated kinase (ERK1/2) pathway, CFM-2 reduced phosphorylation of cAMP-responsive element-binding protein (CREB), suppressed expression of cyclin D1, upregulated the cell cycle regulators and tumor suppressor proteins p21 and p53 and decreased the number of lung adenocarcinoma cells in G2 and S phases of the cell cycle.
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 [1]. CFM-2 has been proven to possess anticonvulsant activity in various models of seizures [2]. 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 [4].
Molecular Weight 311.34
Formula C17H17N3O3
CAS No. 178616-26-7

Storage

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

Solubility Information

DMSO: 45mg/mL (144.5mM)

TargetMolReferences and Literature

1. De Sarro G, et al. Effects of some AMPA receptor antagonists on the development of tolerance in epilepsy-prone rats and in pentylenetetrazole kindled rats. Eur J Pharmacol. 1999 Mar 5;368(2-3):149-59. 2. Rizzo M, et al. Determination of new 2,3-benzodiazepines in rat plasma using high-performance liquid chromatography with ultraviolet detection. J Chromatogr B Biomed Sci Appl. 1999 Aug 20;731(2):207-15. 3. Stepulak A, et al. AMPA antagonists inhibit the extracellular signal regulated kinase pathway and suppress lung cancer growth. Cancer Biol Ther. 2007 Dec;6(12):1908-15. 4. Park JS, et al. Role of spinal cord alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors in complete Freund's adjuvant-induced inflammatory pain. Mol Pain. 2008 Dec 30;4:67.

Related compound libraries

This product is contained In the following compound libraries:
Neurotransmitter Receptor Compound Library Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Anti-Cancer Compound Library

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Keywords

CFM-2 178616-26-7 Membrane transporter/Ion channel Neuroscience iGluR CFM2 CFM 2 inhibitor inhibit

 

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