N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepines such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calcium channels with IC50s of 55 µM and 37 µM for Cav1.2 and Cav1.3, respectively.

Physicochemical Properties

Molecular Formula	C15H10CLFN2O
Molecular Weight	288.70
Exact Mass	288.046
CAS #	2886-65-9
PubChem CID	4540
Appearance	White to off-white solid powder
Density	1.4±0.1 g/cm3
Boiling Point	463.5±55.0 °C at 760 mmHg
Melting Point	204-206°C
Flash Point	234.1±31.5 °C
Vapour Pressure	0.0±1.2 mmHg at 25°C
Index of Refraction	1.648
LogP	2.4
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	1
Heavy Atom Count	20
Complexity	415
Defined Atom Stereocenter Count	0
SMILES	ClC1C([H])=C([H])C2=C(C=1[H])C(C1=C([H])C([H])=C([H])C([H])=C1F)=NC([H])([H])C(N2[H])=O
InChi Key	UVCOILFBWYKHHB-UHFFFAOYSA-N
InChi Code	InChI=1S/C15H10ClFN2O/c16-9-5-6-13-11(7-9)15(18-8-14(20)19-13)10-3-1-2-4-12(10)17/h1-7H,8H2,(H,19,20)
Chemical Name	7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1,4-benzodiazepin-2-one
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	Cav1.2 55 μM (IC50) CaV1.3 37 μM (IC50)
ln Vitro	N-Desalkylflurazepam, a long-acting metabolite of flurazepam, lowers the amplitudes of each component of an evoked potential (EP)[1].
ADME/Pharmacokinetics	Metabolism / Metabolites N-Desalkyl-2-oxoquazepam is a known human metabolite of 2-oxoquazepam.
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. [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.
Additional Infomation	Desalkylflurazepam is a benzodiazepine. See also: Didesethylflurazepam (annotation moved to).

Solubility Data

Solubility (In Vitro)

DMSO: 100 mg/mL (346.38 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (8.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (8.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.4638 mL	17.3190 mL	34.6380 mL
	5 mM	0.6928 mL	3.4638 mL	6.9276 mL
	10 mM	0.3464 mL	1.7319 mL	3.4638 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.