Art. -Nr.: HY-B0168A

Milnacipran hydrochloride

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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

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Reinheit: 99.71%
CAS. Nr.: 101152-94-7
Formel: C₁₅H₂₃ClN₂O
Molecular Weight:282.81

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Milnacipran hydrochloride Chemical Structure

CAS. Nr.: 101152-94-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

norepinephrine transporter and the serotonin transporter (K_i values of 31 and 8.5 nM, respectively)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.05 μM Compound: Milnacipran	Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells	[PMID: 34112854]
HEK293	IC₅₀	0.05 μM Compound: Milnacipran	Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586 Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586	[PMID: 34112854]

In Vitro

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

In Vivo

Milnacipran (30-60 mg/kg; p.o.; single dose) hydrochloride shows anxiolytic effects in rats^[2].
Milnacipran (30-120 mg/kg; p.o.) hydrochloride 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) hydrochloride suppresses hyperalgesia in a dose-dependent manner in mice with intrathecal NMDA-induced thermal hyperalgesia^[5].
Milnacipran (3-30 mg/kg; i.p.) hydrochloride suppresses impulsive, aggressive, and depressive-like behaviors in male C57BL/6N mice^[6].
Milnacipran (20-60 mg/kg; i.p.) hydrochloride suppresses food intake in fasted male C57BL/6J and A^y 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) hydrochloride 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).

Chemical Information

CAS. Nr. 101152-94-7
Appearance Solid
Molecular Weight 282.81
Formel C₁₅H₂₃ClN₂O
Color White to off-white
SMILES

O=C([C@@]1(C2=CC=CC=C2)[C@@H](CN)C1)N(CC)CC.Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (2)

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Journal Impact Factor

Cell Rep Med

Gut microbe-derived milnacipran enhances tolerance to gut ischemia/reperfusion injury. [Abstract]

2023 Mar 21;4(3):100979. PMID: 36948152
Int Immunopharmacol

Innovative role of the antidepressant imipramine in esophageal squamous cell carcinoma treatment: Promoting apoptosis and protective autophagy. [Abstract]

2025 Jan 6:147:113969. PMID: 39764996

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : ≥ 100 mg/mL (353.59 mM)

DMSO : ≥ 48 mg/mL (169.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

3.5359 mL

17.6797 mL

35.3594 mL

5 mM

0.7072 mL

3.5359 mL

7.0719 mL

10 mM

0.3536 mL

1.7680 mL

3.5359 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

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

Mass

Konzentration

Volumen

Molecular Weight

Verdünnungsrechner

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

Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)}

Konzentration _{(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 (8.84 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (8.84 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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (8.84 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.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: PBS

Solubility: 110 mg/mL (388.95 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
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.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (420 KB)
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- Portuguese - PT (420 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]. Chen C, et al. Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9. [Content Brief]

[2]. Mochizuki D, et al. Neurochemical and behavioural characterization of milnacipran, a serotonin and noradrenaline reuptake inhibitor in rats. Psychopharmacology (Berl). 2002 Jul;162(3):323-32. [Content Brief]

[3]. Ueta K, et al. In vitro inhibition of recombinant ligand-gated ion channels by high concentrations of milnacipran. Psychopharmacology (Berl). 2004 Sep;175(2):241-6. [Content Brief]

[4]. Suzuki T, et al. Antiallodynic and antihyperalgesic effect of milnacipran in mice with spinal nerve ligation. Anesth Analg. 2008 Apr;106(4):1309-15, table of contents. [Content Brief]

[5]. Kohno T, et al. Milnacipran inhibits glutamatergic N-methyl-D-aspartate receptor activity in spinal dorsal horn neurons. Mol Pain. 2012 Jun 19;8:45. [Content Brief]

[6]. Tsutsui-Kimura I, et al. Milnacipran affects mouse impulsive, aggressive, and depressive-like behaviors in a distinct dose-dependent manner. J Pharmacol Sci. 2017 Jul;134(3):181-189. [Content Brief]

[7]. Nonogaki K, et al. Milnacipran, a serotonin and norepinephrine reuptake inhibitor, induces appetite-suppressing effects without inducing hypothalamic stress responses in mice. Am J Physiol Regul Integr Comp Physiol. 2007 May;292(5):R1775-81. [Content Brief]

[8]. Andoh T, et al. Milnacipran inhibits itch-related responses in mice through the enhancement of noradrenergic transmission in the spinal cord. J Pharmacol Sci. 2013;123(2):199-202. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	3.5359 mL	17.6797 mL	35.3594 mL	88.3986 mL
	5 mM	0.7072 mL	3.5359 mL	7.0719 mL	17.6797 mL
	10 mM	0.3536 mL	1.7680 mL	3.5359 mL	8.8399 mL
	15 mM	0.2357 mL	1.1786 mL	2.3573 mL	5.8932 mL
	20 mM	0.1768 mL	0.8840 mL	1.7680 mL	4.4199 mL
	25 mM	0.1414 mL	0.7072 mL	1.4144 mL	3.5359 mL
	30 mM	0.1179 mL	0.5893 mL	1.1786 mL	2.9466 mL
	40 mM	0.0884 mL	0.4420 mL	0.8840 mL	2.2100 mL
	50 mM	0.0707 mL	0.3536 mL	0.7072 mL	1.7680 mL
	60 mM	0.0589 mL	0.2947 mL	0.5893 mL	1.4733 mL
	80 mM	0.0442 mL	0.2210 mL	0.4420 mL	1.1050 mL
	100 mM	0.0354 mL	0.1768 mL	0.3536 mL	0.8840 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Milnacipran hydrochloride

2 Cited Publications

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Milnacipran hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Milnacipran hydrochloride

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Milnacipran hydrochloride Related Classifications

Art. -Nr.: HY-B0168A