1. Neuronal Signaling
  2. Serotonin Transporter
  3. Citalopram

Citalopram is a racemate mixture of the active S(+)-enantiomer (Escitalopram; HY-14258) and R(-)-enantiomer. Citalopram is an orally active selective serotonin reuptake inhibitor (SSRI). Citalopram is an antidepressant and enhances serotoninergic neurotransmission.

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Citalopram Chemical Structure

Citalopram Chemical Structure

CAS No. : 59729-33-8

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Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 6 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Citalopram is a racemate mixture of the active S(+)-enantiomer (Escitalopram; HY-14258) and R(-)-enantiomer. Citalopram is an orally active selective serotonin reuptake inhibitor (SSRI). Citalopram is an antidepressant and enhances serotoninergic neurotransmission[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
> 200 μM
Compound: Citalopram
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 32388114]
HEK293 IC50
0.019 μM
Compound: Citalopram
Inhibition of [3H]-serotonin reuptake at human SERT expressed in HEK293 cells after 15 to 20 mins by fluorescence neurotransmitter transporter assay
Inhibition of [3H]-serotonin reuptake at human SERT expressed in HEK293 cells after 15 to 20 mins by fluorescence neurotransmitter transporter assay
[PMID: 21227702]
HEK293 IC50
18.8 μM
Compound: citalopram
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
3.17 nM
Compound: citalopram
Inhibition of [3H]5-HT reuptake at rat SERT expressed in HEK293 cells after 2 mins by liquid scintillation counting
Inhibition of [3H]5-HT reuptake at rat SERT expressed in HEK293 cells after 2 mins by liquid scintillation counting
[PMID: 19717215]
SH-SY5Y IC50
> 200 μM
Compound: Citalopram
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 32388114]
Ventricular myocyte IC50
64.5 μM
Compound: Citalopram
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]
In Vitro

Citalopram (25-175 μM; 24 h) shows a concentration-dependent cytotoxicity[3].
Citalopram (100 μM; 24 h) strongly down-regulates MYBL2, BIRC5, BARD1, AURKA, CCNA2 and CCNE1 in B104 cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[3]

Cell Line: Rat B104, human SH-SY5Y, IMR32 and Kelly neuroblastoma cells
Concentration: 25, 50, 100, 125, 150, 175 μM
Incubation Time: 24 h
Result: Showed a concentration-dependent cytotoxicity.

RT-PCR[3]

Cell Line: B104 cells
Concentration: 100 μM
Incubation Time: 24 h
Result: Strongly down-regulated MYBL2, BIRC5, BARD1, AURKA, CCNA2 and CCNE1 in B104 cells.
In Vivo

Citalopram (5-40 mg/kg; i.p.) reduces immobility time in DBA/2J mice but not in C57BL/6J mice[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6J and DBA/2J mice, aged 5-7 weeks, 16-20 g[4]
Dosage: 5-40 mg/kg
Administration: IP
Result: Reduced immobility time in DBA/2J mice but not in C57BL/6J mice.
Clinical Trial
Molecular Weight

324.39

Formula

C20H21FN2O

CAS No.
Appearance

Oil

Color

Colorless to light yellow

SMILES

N#CC1=CC=C2C(CCCN(C)C)(OCC2=C1)C3=CC=C(C=C3)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (308.27 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 3.0827 mL 15.4135 mL 30.8271 mL
5 mM 0.6165 mL 3.0827 mL 6.1654 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. 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (7.71 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).
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: 99.76%

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. 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 3.0827 mL 15.4135 mL 30.8271 mL 77.0677 mL
5 mM 0.6165 mL 3.0827 mL 6.1654 mL 15.4135 mL
10 mM 0.3083 mL 1.5414 mL 3.0827 mL 7.7068 mL
15 mM 0.2055 mL 1.0276 mL 2.0551 mL 5.1378 mL
20 mM 0.1541 mL 0.7707 mL 1.5414 mL 3.8534 mL
25 mM 0.1233 mL 0.6165 mL 1.2331 mL 3.0827 mL
30 mM 0.1028 mL 0.5138 mL 1.0276 mL 2.5689 mL
40 mM 0.0771 mL 0.3853 mL 0.7707 mL 1.9267 mL
50 mM 0.0617 mL 0.3083 mL 0.6165 mL 1.5414 mL
60 mM 0.0514 mL 0.2569 mL 0.5138 mL 1.2845 mL
80 mM 0.0385 mL 0.1927 mL 0.3853 mL 0.9633 mL
100 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7707 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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Citalopram
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HY-121203
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