Fenobam
Based on 1 Customer Validation
Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.60%
- No. CAS: 57653-26-6
- Fòrmula: C11H11ClN4O2
- Peso molecular:266.68
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Orally Active Compound Library
HY-L061
-
Neurotransmitter Receptor Compound Library
HY-L062
-
Neuroprotective Compound Library
HY-L070
-
Anti-Parkinson's Disease Compound Library
HY-L085
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Antidepressant Compound Library
HY-L108
-
Human Metabolite Library
HY-L123
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Mitochondrial Toxicity Compound Library
HY-L155
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Lactylation Compound Library
HY-L249
-
Apoptosis Compound Library
HY-L003
-
GPCR/G Protein Compound Library
HY-L006
-
Neuronal Signaling Compound Library
HY-L013
-
Anti-Cancer Compound Library
HY-L025
-
CNS-Penetrant Compound Library
HY-L028
Actividad biológica
|
mGluR5 84 nM (IC50) |
rat mGluR5 54 nM (Kd) |
human mGluR5 31 nM (Kd) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
43 nM
Compound: 3, Fenobam
|
Antagonist activity at human mGluR5 expressed in CHO-K1 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization
Antagonist activity at human mGluR5 expressed in CHO-K1 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization
|
[PMID: 22523618] |
| HEK293 | IC50 |
51 nM
Compound: Fenobam
|
Displacement of [3H]-MPEP from human mGlu5 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting analysis
Displacement of [3H]-MPEP from human mGlu5 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting analysis
|
[PMID: 26774652] |
| HEK293 | IC50 |
51 nM
Compound: Fenobam
|
Displacement of [3H]-MPEP from rat mGlu5 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting analysis
Displacement of [3H]-MPEP from rat mGlu5 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting analysis
|
[PMID: 26774652] |
Fenobam (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.
-
Cell Line:LM7 cells
-
Concentration:300 μM
-
Incubation Time:72 h
-
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.
-
Animal Model:Male Long-Evans rats (250-300 g)[3].
-
Dosage:30-60 mg/kg
-
Administration:Oral administration; 3 times a week.
-
Result:Inhibited self-administration.
Chemical Information
-
No. CAS 57653-26-6
-
Appearance Solid
-
Peso molecular 266.68
-
Fòrmula C11H11ClN4O2
-
Color White to off-white
-
SMILES
O=C(NC1=NC(CN1C)=O)NC2=CC=CC(Cl)=C2
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (374.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
-
Ficha de datos (272 KB)
-
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7498 mL | 18.7491 mL | 37.4981 mL | 93.7453 mL |
| 5 mM | 0.7500 mL | 3.7498 mL | 7.4996 mL | 18.7491 mL | |
| 10 mM | 0.3750 mL | 1.8749 mL | 3.7498 mL | 9.3745 mL | |
| 15 mM | 0.2500 mL | 1.2499 mL | 2.4999 mL | 6.2497 mL | |
| 20 mM | 0.1875 mL | 0.9375 mL | 1.8749 mL | 4.6873 mL | |
| 25 mM | 0.1500 mL | 0.7500 mL | 1.4999 mL | 3.7498 mL | |
| 30 mM | 0.1250 mL | 0.6250 mL | 1.2499 mL | 3.1248 mL | |
| 40 mM | 0.0937 mL | 0.4687 mL | 0.9375 mL | 2.3436 mL | |
| 50 mM | 0.0750 mL | 0.3750 mL | 0.7500 mL | 1.8749 mL | |
| 60 mM | 0.0625 mL | 0.3125 mL | 0.6250 mL | 1.5624 mL | |
| 80 mM | 0.0469 mL | 0.2344 mL | 0.4687 mL | 1.1718 mL | |
| 100 mM | 0.0375 mL | 0.1875 mL | 0.3750 mL | 0.9375 mL |
Fenobam Related Classifications
HY-101478 Related Classifications
Powered by Bioz