3,3'-Difluorobenzaldazine
Based on 1 Customer Validation
3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC50s in the 2 to 5 μM range.
For research use only. We do not sell to patients.
- Purity: 99.44%
- CAS No.: 15332-10-2
- Formula: C14H10F2N2
- Molecular Weight:244.24
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BV-2 | IC50 |
136 μM
Compound: DFB
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Positive allosteric modulator activity at mGluR5 in mouse BV2 cells assessed as inhibition of nitric oxide production pre-treated 1 hr before lipopolysaccharide stimulation and measured 24 hrs post lipopolysaccharide stimulation by Griess reagent assay
Positive allosteric modulator activity at mGluR5 in mouse BV2 cells assessed as inhibition of nitric oxide production pre-treated 1 hr before lipopolysaccharide stimulation and measured 24 hrs post lipopolysaccharide stimulation by Griess reagent assay
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[PMID: 25801156] |
| BV-2 | IC50 |
136 μM
Compound: DFB
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Positive allosteric modulation at mGluR5 in mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess assay
Positive allosteric modulation at mGluR5 in mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess assay
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[PMID: 25937015] |
| CHO | EC50 |
2.36 nM
Compound: 1
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Effective concentration against metabotropic glutamate receptor 5 of human transfected into CHO cells
Effective concentration against metabotropic glutamate receptor 5 of human transfected into CHO cells
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[PMID: 15537338] |
| CHO | EC50 |
2.6 μM
Compound: 16
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Positive allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate reader
Positive allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate reader
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[PMID: 25180768] |
3,3'-Difluorobenzaldazine (DFB) causes a concentration-dependent potentiation of the response of human mGluR5 CHO cells to 300 nM glutamate in this assay. The maximal potentiation at this concentration of glutamate is approximately 3.1-fold, with an EC50 for potentiation of 2.6 μM. 3,3'-Difluorobenzaldazine causes similar potentiation of the responses of both human mGluR5 and rat mGluR5 CHO cells to glutamate, quisqualate, and DHPG with comparable potencies[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NMRI and ICR mice (8-9 weeks, 33-40 g)[2]
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Dosage:40-100 nmol (~9.7-24.4 μg)
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Administration:ICV
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Result:Attenuated the locomotor hyperactivity, motor incoordination, and cognitive impairment induced by Ketamine.
Chemical Information
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CAS No. 15332-10-2
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Appearance Solid
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Molecular Weight 244.24
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Formula C14H10F2N2
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Color White to yellow
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SMILES
FC1=CC(/C=N/N=C/C2=CC=CC(F)=C2)=CC=C1
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Synonyms
DFB
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (102.36 mM; ultrasonic and warming and heat to 60°C; 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)
Purity & Documentation
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Data Sheet (270 KB)
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SDS (759 KB)
- English - EN (759 KB)
- Français - FR (759 KB)
- Deutsch - DE (759 KB)
- Norwegian - NO (759 KB)
- Español - ES (759 KB)
- Swedish - SV (759 KB)
- Italian - IT (759 KB)
- Korean - KR (759 KB)
- Portuguese - PT (759 KB)
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Handling Instructions (2659 KB)
References
[1]. O'Brien JA, et al, Chen TB, et al. A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol Pharmacol. 2003;64(3):731-740. [Content Brief]
[2]. Chan MH, et al. Attenuation of ketamine-evoked behavioral responses by mGluR5 positive modulators in mice. Psychopharmacology (Berl). 2008 May;198(1):141-8. [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 | 4.0943 mL | 20.4717 mL | 40.9433 mL | 102.3583 mL |
| 5 mM | 0.8189 mL | 4.0943 mL | 8.1887 mL | 20.4717 mL | |
| 10 mM | 0.4094 mL | 2.0472 mL | 4.0943 mL | 10.2358 mL | |
| 15 mM | 0.2730 mL | 1.3648 mL | 2.7296 mL | 6.8239 mL | |
| 20 mM | 0.2047 mL | 1.0236 mL | 2.0472 mL | 5.1179 mL | |
| 25 mM | 0.1638 mL | 0.8189 mL | 1.6377 mL | 4.0943 mL | |
| 30 mM | 0.1365 mL | 0.6824 mL | 1.3648 mL | 3.4119 mL | |
| 40 mM | 0.1024 mL | 0.5118 mL | 1.0236 mL | 2.5590 mL | |
| 50 mM | 0.0819 mL | 0.4094 mL | 0.8189 mL | 2.0472 mL | |
| 60 mM | 0.0682 mL | 0.3412 mL | 0.6824 mL | 1.7060 mL | |
| 80 mM | 0.0512 mL | 0.2559 mL | 0.5118 mL | 1.2795 mL | |
| 100 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0236 mL |
3,3'-Difluorobenzaldazine Related Classifications
HY-14611 Related Classifications
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