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Dextromilnacipran [96847-55-1]

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Référence NB-64-15133-25mg

Conditionnement : 25mg

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Dextromilnacipran

(Synonyms: Levomilnacipran) Copy Product Info

Synonyms: Levomilnacipran

Catalog No. T2594 Copy Product Info

Purity: >99.99%

Dextromilnacipran (Levomilnacipran) is a selective serotonin and norepinephrine reuptake inhibitor.

Cas No. 96847-55-1

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.5%

Product Information

Dextromilnacipran AI Summary

**Dextromilnacipran** is a pharmacologically active compound primarily studied for its interactions with neurotransmitter transporters, demonstrating significant inhibition of the norepinephrine transporter (NET) and moderate inhibition of the serotonin transporter (SERT). It exhibits potent inhibition of human NET with an IC50 as low as 77.0 nM and moderate inhibition of human SERT with IC50 values ranging between 100.0 nM and 420.0 nM across different studies. The compound shows weaker inhibition of the dopamine transporter (DAT) with an IC50 of 6100.0 nM. Pharmacokinetically, Dextromilnacipran has high oral bioavailability in humans at 84%, with a rapid Tmax of 2.0 hours and a moderate half-life of 8.0 hours. It demonstrates moderate protein binding in human plasma (13.0%) and significant excretion activity in human urine (>80.0%). The compound shows metabolic stability in both human and rat liver microsomes, with clearance values of 3.1 mL.min-1.kg-1 and 24.0 mL.min-1.kg-1 respectively, and exhibits low affinity for P-glycoprotein-mediated transport. Additionally, it has a Log D value of 0.2, indicating moderate lipophilicity, and shows favorable permeability in Caco-2 cell lines. Despite its effective bioactivity, Dextromilnacipran exhibits moderate liver toxicity, indicated by a severity class index of 7.0 for drug-induced liver injury, and shows potential hepatotoxic effects without significant chronic liver disease or tumor formation. Overall, Dextromilnacipran holds promise for modulating neurotransmitter transporters, especially NET and SERT, with potential therapeutic implications and significant pharmacokinetic and pharmacodynamic profiles that warrant further investigation..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Dextromilnacipran (Levomilnacipran) is a selective serotonin and norepinephrine reuptake inhibitor.
Targets & IC50	α-adrenoceptor:3.4 μM (IC50)
Synonyms	Levomilnacipran

Chemical Properties

Molecular Weight	246.35
Formula	C₁₅H₂₂N₂O
Cas No.	96847-55-1
Smiles	C(N(CC)CC)(=O)[C@]1([C@@H](CN)C1)C2=CC=CC=C2
Relative Density.	1.077

Storage & Solubility Information

Storage

Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (1014.82 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Saline: 10 mg/mL (40.59 mM), Solution.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	4.0593 mL	20.2963 mL	40.5927 mL	202.9633 mL
5 mM	0.8119 mL	4.0593 mL	8.1185 mL	40.5927 mL
10 mM	0.4059 mL	2.0296 mL	4.0593 mL	20.2963 mL
20 mM	0.2030 mL	1.0148 mL	2.0296 mL	10.1482 mL
50 mM	0.0812 mL	0.4059 mL	0.8119 mL	4.0593 mL
100 mM	0.0406 mL	0.2030 mL	0.4059 mL	2.0296 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.