2. Neuronal Signaling Cell Cycle/DNA Damage
  3. Serotonin Transporter PERK
  4. Milnacipran

Milnacipran is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran inhibits pERK1/2 activation. Milnacipran has antidepressant, anxiolytic and analgesic properties. Milnacipran inhibits biting behavior in mice. Milnacipran can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia).

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Milnacipran

Milnacipran Chemical Structure

CAS No. : 92623-85-3

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Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

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Milnacipran Related Antibodies

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Description

Milnacipran is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran inhibits pERK1/2 activation. Milnacipran has antidepressant, anxiolytic and analgesic properties. Milnacipran inhibits biting behavior in mice. Milnacipran can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia)[1][2][3][4][5][6][7][8].

In Vitro

Milnacipran shows high affinity for 5-HT and NA transporters (Ki = 8.5 and 31 nM, respectively)[2].
Milnacipran (10-100 µM; 3 min) reduces the amplitude of NMDA (HY-17551)-induced currents in rat spinal lamina II neurons[5].
Milnacipran (100 µM; 10 min) suppresses NMDA (HY-17551)-induced pERK1/2 activation in superficial dorsal horn neurons[5].

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

Milnacipran Related Antibodies
In Vivo

Milnacipran (30-60 mg/kg; p.o.; single dose) shows anxiolytic effects in rats[2].
Milnacipran (30-120 mg/kg; p.o.) increases withdrawal threshold to tactile stimulation and latency to heat stimulation in a dose-dependent manner in rats with spinal nerve ligation (SNL)[4].
Milnacipran (0.01-0.1 µmol; intrathecal) suppresses hyperalgesia in a dose-dependent manner in mice with intrathecal NMDA-induced thermal hyperalgesia[5].
Milnacipran (3-30 mg/kg; i.p.) suppresses impulsive, aggressive, and depressive-like behaviors in male C57BL/6N mice[6].
Milnacipran (20-60 mg/kg; i.p.) suppresses food intake in fasted male C57BL/6J and Ay mice, increases hypothalamic POMC and CART mRNA levels, and does not elevate plasma corticosterone or blood glucose[7].
Milnacipran (0.1-10 μg/site; intrathecal) inhibits Serotonin-induced biting behavior in male ICR mice[8].

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

Animal Model: Male Sprague-Dawley rats; conditioned fear stress test[2]
Dosage: 10, 30, 60 mg/kg
Administration: Oral administration (p.o.), single dose 60 min before testing.
Result: Reduced freezing time at 30 and 60 mg/kg.
Animal Model: Male C57BL/6N mice and male BALB/c mice[6]
Dosage: 0, 3, 10, 30 mg/kg (saline)
Administration: Intraperitoneal injection (i.p.); 60 min prior to each test; single dose per session with washout intervals (1 week for 3-CSRTT, 2 days for RIT).
Result: Reduced premature responses in 3-CSRTT and attack bites in RIT, shortened immobility time in FST (at 10 mg/kg).
Increased aggressive behavior and elevated dopamine levels in the nucleus accumbens (at 30 mg/kg).
Clinical Trial
Molecular Weight

246.35

Formula

C15H22N2O
CAS No.
Appearance

Solid-Liquid Mixture

Color

Colorless to off-white

SMILES

CCN(CC)C([C@@]1(C2=CC=CC=C2)[C@H](C1)CN)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (405.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0593 mL 20.2963 mL 40.5927 mL
5 mM 0.8119 mL 4.0593 mL 8.1185 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (10.15 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (10.15 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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 4.0593 mL 20.2963 mL 40.5927 mL 101.4816 mL
5 mM 0.8119 mL 4.0593 mL 8.1185 mL 20.2963 mL
10 mM 0.4059 mL 2.0296 mL 4.0593 mL 10.1482 mL
15 mM 0.2706 mL 1.3531 mL 2.7062 mL 6.7654 mL
20 mM 0.2030 mL 1.0148 mL 2.0296 mL 5.0741 mL
25 mM 0.1624 mL 0.8119 mL 1.6237 mL 4.0593 mL
30 mM 0.1353 mL 0.6765 mL 1.3531 mL 3.3827 mL
40 mM 0.1015 mL 0.5074 mL 1.0148 mL 2.5370 mL
50 mM 0.0812 mL 0.4059 mL 0.8119 mL 2.0296 mL
60 mM 0.0677 mL 0.3383 mL 0.6765 mL 1.6914 mL
80 mM 0.0507 mL 0.2537 mL 0.5074 mL 1.2685 mL
100 mM 0.0406 mL 0.2030 mL 0.4059 mL 1.0148 mL
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Milnacipran Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Milnacipran92623-85-3Serotonin TransporterPERK5-HTTSERTSLC6A4Protein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasemicethermal hyperalgesiaantidepressantanxiolytic and analgesicsuperficial dorsal horn neuronsRatInhibitorinhibitorinhibit

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