Nortriptyline hydrochloride
Based on 5 publication(s) in Google Scholar
Nortriptyline (Desmethylamitriptyline) hydrochloride, the main active metabolite of Amitriptyline, is a tricyclic antidepressant. Nortriptyline hydrochloride is a potent autophagy inhibitor and has anticancer effects.
For research use only. We do not sell to patients.
- Purity : 99.98%
- CAS No.: 894-71-3
- Formula: C19H22ClN
- Molecular Weight:299.84
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Nortriptyline hydrochloride
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.04 μM
Compound: Nortriptyline
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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] |
In Vitro
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) hydrochloride 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) hydrochloride induces cell cycle arrest and apoptosis in TCCSUP and MBT-2 cells[3].
Nortriptyline (12.55-100 μM; 24 h) hydrochloride 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. Further protocols information, click here.
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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:TCCSUP and MBT-2 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 hours
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Result:Caused cell cycle arrest in these bladder cancer cells.
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Cell Line:TCCSUP and MBT-2 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 hours
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Result:Induced apoptosis in both TCCSUP and MBT-2 cells
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Cell Line:TCCSUP and MBT-2 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 hours
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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.
In Vivo
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.
Chemical Information
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CAS No. 894-71-3
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Appearance Solid
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Molecular Weight 299.84
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Formula C19H22ClN
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Color White to off-white
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SMILES
CNCC/C=C1C2=CC=CC=C2CCC3=CC=CC=C\13.[H]Cl
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Synonyms
Desmethylamitriptyline hydrochloride; Desitriptilina hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
Solvent & Solubility
In Vitro:
DMSO : 70 mg/mL (233.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 7.14 mg/mL (23.81 mM; Need ultrasonic)
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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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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 (sealed storage, away from moisture)
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.
Protocols
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
Purity & Documentation
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Data Sheet (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Dean L. Amitriptyline Therapy and CYP2D6 and CYP2C19 Genotype. Biotechnology Information (US); 2012-2017 Mar 23. [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 (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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.3351 mL | 16.6756 mL | 33.3511 mL | 83.3778 mL |
| 5 mM | 0.6670 mL | 3.3351 mL | 6.6702 mL | 16.6756 mL | |
| 10 mM | 0.3335 mL | 1.6676 mL | 3.3351 mL | 8.3378 mL | |
| 15 mM | 0.2223 mL | 1.1117 mL | 2.2234 mL | 5.5585 mL | |
| 20 mM | 0.1668 mL | 0.8338 mL | 1.6676 mL | 4.1689 mL | |
| DMSO | 25 mM | 0.1334 mL | 0.6670 mL | 1.3340 mL | 3.3351 mL |
| 30 mM | 0.1112 mL | 0.5559 mL | 1.1117 mL | 2.7793 mL | |
| 40 mM | 0.0834 mL | 0.4169 mL | 0.8338 mL | 2.0844 mL | |
| 50 mM | 0.0667 mL | 0.3335 mL | 0.6670 mL | 1.6676 mL | |
| 60 mM | 0.0556 mL | 0.2779 mL | 0.5559 mL | 1.3896 mL | |
| 80 mM | 0.0417 mL | 0.2084 mL | 0.4169 mL | 1.0422 mL | |
| 100 mM | 0.0334 mL | 0.1668 mL | 0.3335 mL | 0.8338 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.