Art. -Nr.: HY-135556

Norfluoxetine

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Norfluoxetine is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K₂P potassium channel inhibitor. Norfluoxetine exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine inhibits high-threshold voltage-gated Ca²⁺ currents in neurons with an EC₅₀ of 20.4 μM. Norfluoxetine can be used in research related to depression, ischemic stroke, and epilepsy.

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Reinheit: 98.71%
CAS. Nr.: 83891-03-6
Formel: C₁₆H₁₆F₃NO
Molecular Weight:295.30

Speicherung:

Store at room temperature, keep dry and cool.

In solvent -80°C, 1 year , -20°C, 6 months

Norfluoxetine Chemical Structure

CAS. Nr.: 83891-03-6

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.8 μM Compound: 40	Inhibition of rat voltage-gated K channel 3.1 expressed in CHO cells by patch clamp assay Inhibition of rat voltage-gated K channel 3.1 expressed in CHO cells by patch clamp assay	[PMID: 23121096]

In Vitro

Norfluoxetine (0.1-10 μM; 12-24 h) inhibits full-length human TREK-2 channels expressed in Xenopus laevis oocytes with an IC₅₀ of 2.7 μM at +40 mV; inhibition is reduced by TPA and ML335 but not by tetraethylammonium or 2-APB^[1].
Norfluoxetine (10-100 μM) reduces single-channel open probability, current amplitude, mean open time, and mean short closed time of truncated human TREK-2 channels reconstituted in lipid bilayers, with increased inhibitory efficacy at voltages above +60 mV, and exhibits similar inhibitory efficacy in high-P_o and standard gating modes^[1].
Norfluoxetine (10 μM) significantly attenuates nitric oxide and TNF release from lipopolysaccharide-activated primary rat microglia^[2].
Norfluoxetine (10-30 μM) reduces protein levels in non-activated primary rat microglia in a dose-dependent manner^[2].
Norfluoxetine (10-30 μM) reduces viability of non-activated primary rat microglia in a dose-dependent manner^[2].
Norfluoxetine (10 μM) significantly increases the number of dead non-activated primary rat microglia, as measured by live/dead nuclear staining^[2].
Norfluoxetine (10 μM) significantly increases the percentage of non-activated primary rat microglia expressing the apoptotic marker cleaved-caspase 3^[2].
Norfluoxetine (10-20 μM; 24 h) induces apoptosis in non-activated primary rat microglia by increasing cleaved-caspase 3 and decreasing full-length caspase 3, without altering caspase 8 levels^[2].
Norfluoxetine (1-100 μM; 30 s) concentration-dependently inhibits voltage-gated Ca²⁺ channel-mediated Ba²⁺ currents in isolated rat cochlear neurons with an EC₅₀ of 20.4 μM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

non-activated primary rat microglia
Concentration:

10 and 20 μM
Incubation Time:

24 h
Result:

Elevated Cleaved-Caspase 3.

In Vivo

Norfluoxetine (5-20 mg/kg; s.c.; single dose) exerts significant dose-dependent anticonvulsant effects in pentylenetetrazol-induced mouse epilepsy^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

CFLP (male, 23 g)^[3]
Dosage:

5 mg/kg; 10 mg/kg; 20 mg/kg
Administration:

s.c.; single dose
Result:

Increased survival rate, survival duration, and seizure latency significantly at 20 mg/kg compared to pentylenetetrazol-only controls.
Increased combined protection score significantly at 10 mg/kg and 20 mg/kg compared to controls.
Showed no significant differences in anticonvulsant effects compared to fluoxetine at matching doses.

Chemical Information

CAS. Nr. 83891-03-6
Appearance Liquid (Density: 1.205±0.06 g/cm³)
Molecular Weight 295.30
Formel C₁₆H₁₆F₃NO
Color Colorless to light yellow
SMILES

FC(F)(F)C(C=C1)=CC=C1OC(C2=CC=CC=C2)CCN
Structure Classification
- Others
Initial Source
- Animals
- Endogenous metabolite
human plasma
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Store at room temperature, keep dry and cool

In solvent	-80°C	1 year
	-20°C	6 months

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (338.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3864 mL

16.9319 mL

33.8639 mL

5 mM

0.6773 mL

3.3864 mL

6.7728 mL

10 mM

0.3386 mL

1.6932 mL

3.3864 mL

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.47 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Proks P, et al. Norfluoxetine inhibits TREK-2 K2P channels by multiple mechanisms including state-independent effects on the selectivity filter gate. The Journal of general physiology. 2021 Aug 02;153(8):e202012812. [Content Brief]

[2]. Dhami KS, et al. Fluoxetine and its metabolite norfluoxetine induce microglial apoptosis. Journal of neurochemistry. 2019 Mar;148(6):761-778. [Content Brief]

[3]. Kecskeméti V, et al. Norfluoxetine and fluoxetine have similar anticonvulsant and Ca2+ channel blocking potencies. Brain research bulletin. 2005 Sep 30;67(1-2):126-32. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.3864 mL	16.9319 mL	33.8639 mL	84.6597 mL
	5 mM	0.6773 mL	3.3864 mL	6.7728 mL	16.9319 mL
	10 mM	0.3386 mL	1.6932 mL	3.3864 mL	8.4660 mL
	15 mM	0.2258 mL	1.1288 mL	2.2576 mL	5.6440 mL
	20 mM	0.1693 mL	0.8466 mL	1.6932 mL	4.2330 mL
	25 mM	0.1355 mL	0.6773 mL	1.3546 mL	3.3864 mL
	30 mM	0.1129 mL	0.5644 mL	1.1288 mL	2.8220 mL
	40 mM	0.0847 mL	0.4233 mL	0.8466 mL	2.1165 mL
	50 mM	0.0677 mL	0.3386 mL	0.6773 mL	1.6932 mL
	60 mM	0.0564 mL	0.2822 mL	0.5644 mL	1.4110 mL
	80 mM	0.0423 mL	0.2116 mL	0.4233 mL	1.0582 mL
	100 mM	0.0339 mL	0.1693 mL	0.3386 mL	0.8466 mL

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Norfluoxetine

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Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Norfluoxetine Related Classifications

HY-135556 Related Classifications