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

ミルナシプラン塩酸塩  (Synonyms: Milnacipran (hydrochloride))

製品番号: HY-B0168A 純度: 99.71%
COA 取扱説明書 Technical Support

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 (Ki 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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Milnacipran hydrochloride

ミルナシプラン塩酸塩 構造式

CAS 番号 : 101152-94-7

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 33 在庫あり
Solution
10 mM * 1 mL in DMSO USD 33 在庫あり
Solid
5 mg $30 在庫あり
10 mg $40 在庫あり
25 mg $70 在庫あり
50 mg $100 在庫あり
100 mg $180 在庫あり
200 mg   お問い合わせ  
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* アイテムを追加する前、数量をご選択ください

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Based on 2 publication(s) in Google Scholar

Other Forms of Milnacipran hydrochloride:

ミルナシプラン塩酸塩 関連抗体

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製品説明

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 (Ki 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)[1][2][3][4][5][6][7][8].

IC50 & Target

norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively)
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.05 3
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]
HEK293 IC50
0.05 3
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]
HEK293 IC50
0.05 3
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]
体外実験

Milnacipran hydrochloride shows high affinity for 5-HT and NA transporters (Ki = 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.

ミルナシプラン塩酸塩 関連抗体
体内実験

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 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) 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).
分子量

282.81

分子式

C15H23ClN2O
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
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 (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.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

V1

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濃度 （終了）

C2

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体積 （終了）

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体内:

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 (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.

    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 (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.

    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.

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.
Calculation results:
Working solution concentration: 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).
純度とドキュメンテーション
参考文献

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 (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.

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.

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Milnacipran hydrochloride Related Classifications

  • Molarity Calculator

  • Dilution Calculator

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

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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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    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:

Milnacipran101152-94-7Serotonin TransporterPERK5-HTTSERTSLC6A4Protein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasemicethermal hyperalgesiaantidepressantanxiolytic and analgesicsuperficial dorsal horn neuronsRatInhibitorinhibitorinhibit

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