ミルナシプラン塩酸塩
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 (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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.71%
- CAS 番号: 101152-94-7
- 分子式: C15H23ClN2O
- 分子量:282.81
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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)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Milnacipran hydrochloride
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生物活性
norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.05 μM
Compound: Milnacipran
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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
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[PMID: 34112854] |
| HEK293 | IC50 |
0.05 μM
Compound: Milnacipran
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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
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[PMID: 34112854] |
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.
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.
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Animal Model:Male Sprague-Dawley rats; conditioned fear stress test[2]
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Dosage:10, 30, 60 mg/kg
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Administration:Oral administration (p.o.), single dose 60 min before testing.
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Result:Reduced freezing time at 30 and 60 mg/kg.
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Animal Model:Male C57BL/6N mice and male BALB/c mice[6]
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Dosage:0, 3, 10, 30 mg/kg (saline)
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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)
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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).
化学情報
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CAS 番号 101152-94-7
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性状 Solid
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分子量 282.81
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分子式 C15H23ClN2O
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Color White to off-white
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SMILES
O=C([C@@]1(C2=CC=CC=C2)[C@@H](CN)C1)N(CC)CC.Cl
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別名
Milnacipran (hydrochloride)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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)
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
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
溶剤 & 溶解度
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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
Add each solvent one by one: PBS
Solubility: 110 mg/mL (388.95 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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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.
純度とドキュメンテーション
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データシート (282 KB)
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SDS (420 KB)
- English - EN (420 KB)
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- Deutsch - DE (420 KB)
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- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Portuguese - PT (420 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
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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