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Amitriptyline is a common oral anticholinergic. Amitriptyline has anticholinergic properties. Amitriptyline can be used to quantify anticholinergic adverse reactions in patients taking amitriptyline and placebo .

For research use only. We do not sell to patients.

Amitriptyline Chemical Structure

Amitriptyline Chemical Structure

CAS No. : 50-48-6

Size Price Stock Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Liquid
10 mg USD 50 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Amitriptyline:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Amitriptyline is a common oral anticholinergic. Amitriptyline has anticholinergic properties. Amitriptyline can be used to quantify anticholinergic adverse reactions in patients taking amitriptyline and placebo [1].

Cellular Effect
Cell Line Type Value Description References
CHO IC50
3 μM
Compound: Amitryptline
Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by whole-cell patch clamp assay
Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by whole-cell patch clamp assay
[PMID: 30653317]
CHO-K1 IC50
1.6 μM
Compound: amitriptyline
Inhibition of human NaV1.5 alpha subunit expressed in CHOK1 cells at -90 mV holding potential by patch clamp electrophysiological assay
Inhibition of human NaV1.5 alpha subunit expressed in CHOK1 cells at -90 mV holding potential by patch clamp electrophysiological assay
[PMID: 22770500]
CHO-K1 IC50
3.1 μM
Compound: amitriptyline
Inhibition of human NaV1.2 alpha subunit expressed in CHOK1 cells at -65 mV holding potential by patch clamp electrophysiological assay
Inhibition of human NaV1.2 alpha subunit expressed in CHOK1 cells at -65 mV holding potential by patch clamp electrophysiological assay
[PMID: 22770500]
HEK293 IC50
1 μM
Compound: amitriptyline
Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay
Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay
[PMID: 22770500]
HEK293 IC50
12 μM
Compound: amitriptyline
Inhibition of human NaV1.7 F1737A mutant expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay
Inhibition of human NaV1.7 F1737A mutant expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay
[PMID: 22770500]
HEK293 IC50
16.9 μM
Compound: amitriptyline
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
[PMID: 18788725]
HEK293 IC50
7 μM
Compound: amitriptyline
Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -90 mV holding potential by patch clamp electrophysiological assay
Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -90 mV holding potential by patch clamp electrophysiological assay
[PMID: 22770500]
HEK293 IC50
9.6 μM
Compound: Amitriptyline
Inhibition of [3H]-dofetilide binding to human ERG expressed in HEK293 cell membranes measured after 1 hr by liquid scintillation counting method
Inhibition of [3H]-dofetilide binding to human ERG expressed in HEK293 cell membranes measured after 1 hr by liquid scintillation counting method
[PMID: 30597328]
HepG2 IC50
29.6 μM
Compound: Amitriptyline
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by measuring ATP content incubated for 24 hrs by luminescent analysis
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by measuring ATP content incubated for 24 hrs by luminescent analysis
[PMID: 32442850]
NCI-H1650 GI50
> 40 μM
Compound: Amitriptyline
Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay
[PMID: 26372073]
SH-SY5Y IC50
48.1 μM
Compound: Amitriptyline
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability by measuring ATP content incubated for 24 hrs by luminescent analysis
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability by measuring ATP content incubated for 24 hrs by luminescent analysis
[PMID: 32442850]
Ventricular myocyte IC50
23.2 μM
Compound: Amitriptyline
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
3.75 μM
Compound: Amitriptyline
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
[PMID: 22761000]
Molecular Weight

277.40

Formula

C20H23N

CAS No.
Appearance

Liquid (Density: 1.076±0.06 g/cm3)

Color

Colorless to light yellow

SMILES

CN(CC/C=C1C2=CC=CC=C2CCC3=C\1C=CC=C3)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (360.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6049 mL 18.0245 mL 36.0490 mL
5 mM 0.7210 mL 3.6049 mL 7.2098 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 (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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.01 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 (9.01 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.
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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.94%

References

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 3.6049 mL 18.0245 mL 36.0490 mL 90.1226 mL
5 mM 0.7210 mL 3.6049 mL 7.2098 mL 18.0245 mL
10 mM 0.3605 mL 1.8025 mL 3.6049 mL 9.0123 mL
15 mM 0.2403 mL 1.2016 mL 2.4033 mL 6.0082 mL
20 mM 0.1802 mL 0.9012 mL 1.8025 mL 4.5061 mL
25 mM 0.1442 mL 0.7210 mL 1.4420 mL 3.6049 mL
30 mM 0.1202 mL 0.6008 mL 1.2016 mL 3.0041 mL
40 mM 0.0901 mL 0.4506 mL 0.9012 mL 2.2531 mL
50 mM 0.0721 mL 0.3605 mL 0.7210 mL 1.8025 mL
60 mM 0.0601 mL 0.3004 mL 0.6008 mL 1.5020 mL
80 mM 0.0451 mL 0.2253 mL 0.4506 mL 1.1265 mL
100 mM 0.0360 mL 0.1802 mL 0.3605 mL 0.9012 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

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Amitriptyline
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