Fenobam hydrate
Fenobam hydrate is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction.
For research use only. We do not sell to patients.
- CAS No.: 63540-28-3
- Formula: C11H13ClN4O3
- Molecular Weight:284.70
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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mGluR5 84 nM (IC50) |
human mGluR5 31 nM (Kd) |
rat mGluR5 54 nM (Kd) |
Fenobam hydrate (300 μM; 72 h) significantly inhibits proliferation and induces apoptosis in LM7 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LM7 cells
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Concentration:300 μM
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Incubation Time:72 h
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Result:Significantly reduced total number of cells, proliferating cells, and induced apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Long-Evans rats (250-300 g)[3].
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Dosage:30-60 mg/kg
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Administration:Oral administration; 3 times a week.
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Result:Inhibited self-administration.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 63540-28-3
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Molecular Weight 284.70
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Formula C11H13ClN4O3
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SMILES
O=C(NC1=NC(CN1C)=O)NC2=CC=CC(Cl)=C2.O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Porter RH, et al. Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J Pharmacol Exp Ther. 2005 Nov;315(2):711-21. [Content Brief]
[2]. Liao S, et al. Osteosarcoma cell proliferation and survival requires mGluR5 receptor activity and is blocked by Riluzole. PLoS One. 2017 Feb 23;12(2):e0171256. [Content Brief]
[3]. Keck TM, et al. Fenobam sulfate inhibits cocaine-taking and cocaine-seeking behavior in rats: implications for addiction treatment in humans. Psychopharmacology (Berl). 2013;229(2):253-265. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fenobam hydrate Related Classifications
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