N-Desalkylflurazepam
Based on 1 Customer Validation
N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calcium channels with IC50 values of 55 μM and 37 μM for Cav1.2 and Cav1.3, respectively.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 2886-65-9
- Formula: C15H10ClFN2O
- Molecular Weight:288.70
-
Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
All Calcium Channel Isoforms
More
Biological Activity
|
Cav1.2 55 μM (IC50) |
CaV1.3 37 μM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 2.2.15 | CC50 |
0.183 mM
Compound: 7b
|
Cytotoxicity against human Hep G2.2.15 cells
Cytotoxicity against human Hep G2.2.15 cells
|
[PMID: 18524583] |
| HepG2 2.2.15 | IC50 |
0.294 mM
Compound: 7b
|
Antiviral activity against hepatitis B virus infected Hep G2.2.15 cells assessed as inhibition of HBsAg secretion
Antiviral activity against hepatitis B virus infected Hep G2.2.15 cells assessed as inhibition of HBsAg secretion
|
[PMID: 18524583] |
| HepG2 2.2.15 | IC50 |
5.36 mM
Compound: 7b
|
Antiviral activity against hepatitis B virus infected Hep G2.2.15 cells assessed as inhibition of HBeAg secretion
Antiviral activity against hepatitis B virus infected Hep G2.2.15 cells assessed as inhibition of HBeAg secretion
|
[PMID: 18524583] |
Flurazepam's long-acting metabolite, N-Desalkylflurazepam, reduces the amplitudes of all the evoked potentials (EPs) components[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 2886-65-9
-
Appearance Solid
-
Molecular Weight 288.70
-
Formula C15H10ClFN2O
-
Color White to off-white
-
SMILES
O=C1NC2=C(C(C3=C(F)C=CC=C3)=NC1)C=C(Cl)C=C2
-
Synonyms
Norfludiazepam
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (346.38 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 (protect from light). 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 (protect from light). 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (281 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. J J Kulikowski, et al. Are the amplitudes of visual evoked potentials sensitive indices of hangover effects after repeated doses of benzodiazepines? Psychopharmacology Suppl. 1984;1:154-64. [Content Brief]
[2]. Damien E Earl, et al. Inhibition of recombinant L-type voltage-gated calcium channels by positive allosteric modulators of GABAA receptors. J Pharmacol Exp Ther. 2011 Apr;337(1):301-11. [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 (protect from light). 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 | 3.4638 mL | 17.3190 mL | 34.6380 mL | 86.5951 mL |
| 5 mM | 0.6928 mL | 3.4638 mL | 6.9276 mL | 17.3190 mL | |
| 10 mM | 0.3464 mL | 1.7319 mL | 3.4638 mL | 8.6595 mL | |
| 15 mM | 0.2309 mL | 1.1546 mL | 2.3092 mL | 5.7730 mL | |
| 20 mM | 0.1732 mL | 0.8660 mL | 1.7319 mL | 4.3298 mL | |
| 25 mM | 0.1386 mL | 0.6928 mL | 1.3855 mL | 3.4638 mL | |
| 30 mM | 0.1155 mL | 0.5773 mL | 1.1546 mL | 2.8865 mL | |
| 40 mM | 0.0866 mL | 0.4330 mL | 0.8660 mL | 2.1649 mL | |
| 50 mM | 0.0693 mL | 0.3464 mL | 0.6928 mL | 1.7319 mL | |
| 60 mM | 0.0577 mL | 0.2887 mL | 0.5773 mL | 1.4433 mL | |
| 80 mM | 0.0433 mL | 0.2165 mL | 0.4330 mL | 1.0824 mL | |
| 100 mM | 0.0346 mL | 0.1732 mL | 0.3464 mL | 0.8660 mL |