[CAS NO. 178616-26-7] CFM-2
PRODUCTS SPECIFICATIONS [178616-26-7]
DESCRIPTION [178616-26-7]
Overview
| MDL | MFCD01321072 |
|---|---|
| Molecular Weight | 311.34 |
| Molecular Formula | C17H17N3O3 |
| SMILES | O=C1NN=C(C2=CC=C(N)C=C2)C3=CC(OC)=C(OC)C=C3C1 |
1 Publications Citing Use of MCE
Summary
IC50 & Target
|
AMPA Receptor |
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 number of lung adenocarcinoma cells in G2 and S phases of the cell cycle.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pretreatment with CFM-2 delays the progression of seizure rank during repeated administration of pentylentetrazole. At the end of the period of repeated pentylentetrazole treatment (6 weeks) the mean seizure score was 0 in vehicle treated controls, 4.3 in animals treated with vehicle + pentylentetrazole, 2.2 in rats treated chronically with CFM-2 (20 μmol/kg; i.p.) + pentylentetrazole and 1.0 in rats treated repeatedly with CFM-2 (50 μmol/kg; i.p.) + pentylenetetrazole. CFM-2 is also able to antagonize the long-term increase in sensitivity of the convulsant effects of GABA function inhibitors in pentylentetrazole-kindled animals
[1]
.
Intrathecal application of two selective non-competitive AMPAR antagonists, CFM-2 (25 and 50 μg) and GYKI 52466 (50μg), 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 affects the contralateral basal responses to thermal and mechanical stimuli
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 50 mg/mL ( 160.60 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.2119 mL | 16.0596 mL | 32.1192 mL |
| 5 mM | 0.6424 mL | 3.2119 mL | 6.4238 mL |
| 10 mM | 0.3212 mL | 1.6060 mL | 3.2119 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.75 mg/mL (8.83 mM); Clear solution
References
- [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.
