Nortriptyline
Based on 5 publication(s) in Google Scholar
Nortriptyline (Desmethylamitriptyline), the main active metabolite of Amitriptyline, is a tricyclic antidepressant. Nortriptyline is a potent autophagy inhibitor and has anticancer effects. N
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- Pureté: 99.94%
- CAS No.: 72-69-5
- Formule: C19H21N
- Masse moléculaire:263.38
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Activité biologique
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) Nortriptyline
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
171 μM
Compound: 9c
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Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
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[PMID: 25882526] |
| HEK293 | IC50 |
249 μM
Compound: 9c
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Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
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[PMID: 25882526] |
| HEK293 | IC50 |
270 μM
Compound: 9c
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Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
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[PMID: 25882526] |
| HEK293 | IC50 |
389 μM
Compound: 9c
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Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
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[PMID: 25882526] |
Amitriptyline is metabolized by CYP2C19 to the active metabolite, Nortriptyline. Nortriptyline blocks the reuptake of Norepinephrine more potently than Serotonin[1].
Nortriptyline (6.25-100 μM; 24-72 h) markedly reducs the viability of TCCSUP and mouse MBT-2 bladder cancer cells in a concentration- and time-dependent manner[3].
Nortriptyline (12.55-100 μM; 24 h) induces cell cycle arrest and apoptosis in TCCSUP and MBT-2 cells[3].
Nortriptyline (12.55-100 μM; 24 h) induces both intrinsic and extrinsic apoptosis in these bladder cancer cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human TCCSUP and mouse MBT-2 bladder cancer cells
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Concentration:6.25 μM, 12.5 μM, 25 μM, 50 μM and 100 μM
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Incubation Time:24, 48, or 72 h
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Result:Exhibited cytotoxic effects on TCCSUP and MBT-2 cells.
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Cell Line:Human TCCSUP and mouse MBT-2 bladder cancer cells
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Concentration:25 μM, 50 μM, or 100 μM (TCCSUP); 12.5 μM, 25 μM, or 50 μM (MBT-2 cells)
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Incubation Time:24 h
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Result:Caused cell cycle arrest in these bladder cancer cells.
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Cell Line:Human TCCSUP and mouse MBT-2 bladder cancer cells
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Concentration:25 μM, 50 μM, or 100 μM (TCCSUP); 12.5 μM, 25 μM, or 50 μM (MBT-2 cells)
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Incubation Time:24 h
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Result:Induced apoptosis in both TCCSUP and MBT-2 cells.
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Cell Line:Human TCCSUP and mouse MBT-2 bladder cancer cells
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Concentration:25 μM, 50 μM, or 100 μM (TCCSUP); 12.5 μM, 25 μM, or 50 μM (MBT-2 cells)
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Incubation Time:24 h
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Result:Increased the expression of Fas, FasL, FADD, Bax, Bak, and cleaved forms of caspase-3, caspase-8, caspase-9, and poly(ADP-ribose) polymerase. Decreased the expression of Bcl-2, Bcl-xL, BH3 interacting domain death agonist, X-linked inhibitor of apoptosis protein, and survivin.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male C3H/HeN mice (25-30 g; 2-3 months of age) injected with MBT-2 cells[3]
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Dosage:10 or 20 mg/kg
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Administration:Intraperitoneal injection; every day; for three weeks.
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Result:Suppressed tumor growth in mice inoculated with MBT-2 cells.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 72-69-5
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Appearance Solid
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Masse moléculaire 263.38
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Formule C19H21N
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Color White to off-white
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SMILES
CNCC/C=C1C2=CC=CC=C2CCC3=CC=CC=C\13
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Synonyms
Desmethylamitriptyline; Desitriptilina
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Commun Signal
Tricyclic antidepressants induce liver inflammation by targeting NLRP3 inflammasome activation. [Abstract]2023 May 25;21(1):123. PMID: 37231437 -
J Exp Med
Repurposing a tricyclic antidepressant in tumor and metabolism disease treatment through fatty acid uptake inhibition. [Abstract]2023 Mar 6;220(3):e20221316. PMID: 36520461 -
Int J Biol Macromol
RNA binding motif single-stranded interacting protein 1 drives renal fibrosis by stabilizing Annexin A8 mRNA to activate PI3K/AKT signaling. [Abstract]2026 May 24:368:152687. PMID: 42184845 -
EMBO Mol Med
RBMS1 orchestrates cardiac hypertrophy by facilitating CTTN splice-switching and sarcomere dynamics. [Abstract]2025 Dec;17(12):3555-3585. PMID: 41214391 -
Pharmaceuticals (Basel)
Comparative Pharmacological Profiling of Psychotherapeutic Drugs Reveals a Functional Taxonomy Based on Direct Inhibition of Smooth Muscle Excitability. [Abstract]2026 Apr 21;19(4):645. PMID: 42075900
Solvant et solubilité
DMSO : ≥ 100 mg/mL (379.68 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (9.49 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 (9.49 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (284 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Dean L. Amitriptyline Therapy and CYP2D6 and CYP2C19 Genotype. In: Pratt VM, Scott SA, Pirmohamed M, et al., eds. Medical Genetics Summaries. Bethesda (MD): National Center for Biotechnology Information (US); March 23, 2017. [Content Brief]
[2]. Petrosyan E, et al. Repurposing Autophagy Regulators in Brain Tumors [published online ahead of print, 2022 Feb 18]. Int J Cancer. 2022;10.1002/ijc.33965. [Content Brief]
[3]. Sheau-Yun Yuan, et al. Nortriptyline induces mitochondria and death receptor-mediated apoptosis in bladder cancer cells and inhibits bladder tumor growth in vivo. Eur J Pharmacol. 2015 Aug 15:761:309-20. [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 (protect from light). 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 | 3.7968 mL | 18.9840 mL | 37.9680 mL | 94.9199 mL |
| 5 mM | 0.7594 mL | 3.7968 mL | 7.5936 mL | 18.9840 mL | |
| 10 mM | 0.3797 mL | 1.8984 mL | 3.7968 mL | 9.4920 mL | |
| 15 mM | 0.2531 mL | 1.2656 mL | 2.5312 mL | 6.3280 mL | |
| 20 mM | 0.1898 mL | 0.9492 mL | 1.8984 mL | 4.7460 mL | |
| 25 mM | 0.1519 mL | 0.7594 mL | 1.5187 mL | 3.7968 mL | |
| 30 mM | 0.1266 mL | 0.6328 mL | 1.2656 mL | 3.1640 mL | |
| 40 mM | 0.0949 mL | 0.4746 mL | 0.9492 mL | 2.3730 mL | |
| 50 mM | 0.0759 mL | 0.3797 mL | 0.7594 mL | 1.8984 mL | |
| 60 mM | 0.0633 mL | 0.3164 mL | 0.6328 mL | 1.5820 mL | |
| 80 mM | 0.0475 mL | 0.2373 mL | 0.4746 mL | 1.1865 mL | |
| 100 mM | 0.0380 mL | 0.1898 mL | 0.3797 mL | 0.9492 mL |
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