| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| Other Sizes |
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| ln Vitro |
CYP2C19 helps amitriptyline convert to nortriptyline, which is its active metabolite. When it comes to preventing refeeding from nortriptyline, nortriptyline works better than serotonin [1]. In a concentration- and time-maintained manner, nortriptyline hydrochloride (6.25-100 μM; 24-72 hours) dramatically lowers TCCSUP and bladder MBT-2 bladder viability [3]. In TCCSUP and MBT-2 cells, nortriptyline hydrochloride (12.55-100 μM; 24 hours) can cause cell cycle abduction and cytography [3]. Both the inner and outer cells of the pancreas can develop these colon cancer cells when exposed to nortriptyline hydrochloride (12.55-100 μM; 24) [3]. Vital cycle apoptosis of TCCSUP and MBT-2 cells[3] 25 μM, 50 μM, or 100 μM (TCCSUP); 12.5 μM, 25 μM, or 50 μM (MBT-2 cells) Induces apoptosis of TCCSUP and MBT-2 cells for 24 hours TCCSUP and MBT-2 cells[3] 25 μM, 50 μM, or 100 μM (TCCSUP); 12.5 μM, 25 μM, or 50 μM (MBT-2 cells) 24 hours Increases Fas, FasL, FADD, Bax, Bak, and caspase-3. caspase-8, caspase-9, and polymerase (ADP-ribose). decreases the expression of survivin, X-linked apoptosis protein inhibitor, BH3 interaction domain death agonist, Bcl-2, and Bcl-xL.
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| ln Vivo |
MBT-2 cell tumor development is inhibited by nortriptyline hydrochloride (10–20 mg/kg; intraperitoneal injection; daily; for 3 weeks) [3].
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: Human TCCSUP and Mouse MBT-2 Bladder Cancer Cells Tested Concentrations: 6.25 μM, 12.5 μM, 25 μM, 50 μM and 100 μM Incubation Duration: 24, 48 or 72 hrs (hours) Experimental Results: Cells exhibit Toxic effects on TCCSUP and MBT-2 cells. Cell cycle analysis[3] Cell Types: TCCSUP and MBT-2 Cell Tested Concentrations: 25 μM, 50 μM or 100 μM (TCCSUP); 12.5 μM, 25 μM or 50 μM (MBT-2 cells) Incubation Duration: 24 hrs (hours) Experimental Results: leading to cell cycle arrest in these bladder cancer cells. Apoptosis analysis[3] Cell Types: TCCSUP and MBT-2 Cell Tested Concentrations: 25 μM, 50 μM or 100 μM (TCCSUP); 12.5 μM, 25 μM or 50 μM (MBT-2 cells) Incubation Duration: 24 hrs (hours) Experimental Results: Induction of apoptosis in TCCSUP and MBT-2 cells Western blot analysis [3] Cell Types: TCCSUP and MBT-2 Cell Tested Concentrations: 25 μM, 50 μM or 100 μM (TCCSUP); 12.5 μM, 25 μM or 50 μM (MBT- 2 cells) Incubation Duration: 24 hrs (hours) Experimental Results: Increased expression of Fas, FasL, FADD, Bax, Bak, and cleaved forms of caspase-3, caspase-8, caspase-9, and |
| Animal Protocol |
Animal/Disease Models: Adult male C3H/HeN mice (25-30 g; 2-3 months old) were injected with MBT-2 cells [3]
Doses: 10 or 20 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; three weeks . Experimental Results: Tumor growth was inhibited in mice vaccinated with MBT-2 cells. |
| References |
[1]. Dean L. Amitriptyline Therapy and CYP2D6 and CYP2C19 Genotype. Biotechnology Information (US); 2012-2017 Mar 23.
[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. [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. |
| Molecular Formula |
C19H22CLN
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|---|---|
| Molecular Weight |
299.842
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| Exact Mass |
263.1674
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| CAS # |
894-71-3
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| Related CAS # |
Nortriptyline;72-69-5;Nortriptyline-d3 hydrochloride;203784-52-5
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
Cl[H].N([H])(C([H])([H])[H])C([H])([H])C([H])([H])/C(/[H])=C1\C2=C([H])C([H])=C([H])C([H])=C2C([H])([H])C([H])([H])C2=C([H])C([H])=C([H])C([H])=C2\1
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| Synonyms |
Nortriptyline HCl Lilly 38489 N 7048NortriptylineAllegron DesmethylamitriptylinAventyl Desitriptyline
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~277.91 mM)
H2O : ~7.14 mg/mL (~23.81 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3351 mL | 16.6756 mL | 33.3511 mL | |
| 5 mM | 0.6670 mL | 3.3351 mL | 6.6702 mL | |
| 10 mM | 0.3335 mL | 1.6676 mL | 3.3351 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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