Fenobam |
رقم الكتالوجGC11766
One-Click Copy Product Info
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Fenobam هو مضاد mGluR5 انتقائي ، نشط عن طريق الفم ، يخترق الدماغ يعمل في موقع تعديل خيفي (Kds من 54 و 31 نانومتر لمستقبلات mGlu5 المؤتلفة للفئران والبشر ، على التوالي)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 57653-26-6
Sample solution is provided at 25 µL, 10mM.
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Fenobam is a selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity[1][2].
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.
[2]. Laura F, et al. The Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Fenobam: Pharmacokinetics, Side Effects, and Analgesic Effects in Healthy Human Subjects.bioRxiv 391383;
| Cas No. | 57653-26-6 | SDF | |
| Chemical Name | 1-(3-chlorophenyl)-3-(1-methyl-4-oxo-4,5-dihydro-1H-imidazol-2-yl)urea | ||
| Canonical SMILES | ClC1=CC(NC(NC(N(C)C2)=NC2=O)=O)=CC=C1 | ||
| Formula | C11H11N4O2Cl | M.Wt | 266.69 |
| الذوبان | <26.67mg/ml in DMSO | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7497 mL | 18.7484 mL | 37.4967 mL |
| 5 mM | 749.9 μL | 3.7497 mL | 7.4993 mL |
| 10 mM | 375 μL | 1.8748 mL | 3.7497 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)