2. Membrane Transporter/Ion Channel Neuronal Signaling Stem Cell/Wnt MAPK/ERK Pathway
  3. nAChR ERK p38 MAPK
  4. Varenicline Tartrate

Varenicline Tartrate  (Synonyms: CP 526555-18)

Cat. No.: HY-10021 Purity: 99.93%
Data Sheet
SDS
COA
Handling Instructions Technical Support

Solubility

In Vivo Dissolution Calculator

Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation.

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Varenicline Tartrate Chemical Structure

Varenicline Tartrate Chemical Structure

CAS No. : 375815-87-5

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Based on 1 publication(s) in Google Scholar

Other Forms of Varenicline Tartrate:

Varenicline Tartrate Related Antibodies

Top Publications Citing Use of Products

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

View All p38 MAPK Isoform Specific Products:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation[1][2][3][4][5].

IC50 & Target

IC50: 250 nM (α4β2 nAChR) [2]
In Vitro

Varenicline (200 μM, 24 h) shows no affection to cell viability of HUVEC cells[3].
Varenicline (100 μM, 24 h) lowers expression of VE-cadherin in HUVEC cells as Varenicline (100 μM, 30 min) significantly activates ERK1/2 and p38 signaling[3].
Varenicline (100 μM, 4 h) promotes migration of HUVEC cells by 2.4-fold[3].

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

Varenicline Tartrate Related Antibodies

Cell Viability Assay[3]

Cell Line: HUVEC
Concentration: 100, 200, 300, 500 μM
Incubation Time: 24 h
Result: Did not affect cell viability at 100 and 200 μM (96.8 ± 0.1% and 93.9 ± 1.8%, respectively). Decreased cell viability to 85.7 ± 7.5% and 57.8 ± 7.7% for 300 and 500 μM, respectively.

Western Blot Analysis[3]

Cell Line: HUVEC
Concentration: 100 μM
Incubation Time: 1, 5, 10, 15 ,30 ,60 min, 24 h
Result: Significantly activated ERK1/2 and p38 signaling with peak activity at 10–15 min and 10–30 min after treatment, respectively, lowered expression of VE-cadherin at 24 h. MLA (100 nM) significantly reversed the Varenicline-induced effects.

Cell Migration Assay [3]

Cell Line: HUVEC
Concentration: 100 μM
Incubation Time: 4 h
Result: Significantly increased the number of migrating cells by 2.4-fold compared with vehicle treatment. MLA (100 nM) completely blocked Varenicline-stimulated migration.
In Vivo

Varenicline (0.5, 1mg/kg, s.c., acute administration) dose-dependently reverses Fentanyl-induced respiratory depression in rats while slightly alleviates Fentanyl-induced sedation[4].
Varenicline (0.004–0.04 mg/kg/h, i.v.drip, 23h a day for 7-10 d) dose-dependently reduces self-administration of nicotine alone (0.0032 mg/kg/inj), and in combination with cocaine (0.0032 mg/kg/inj) with no significant effects on food-maintained responding in cocaine- and nicotine-experienced adult rhesus monkeys[5].
Varenicline (0.178-5.6 mg/kg, i.p., acute administration) shows antidepressant-like activity in the forced swim test in C57BL/6J and CD-1 mice[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT04602494Massachusetts General Hospital|National Institute on Drug Abuse (NIDA)
Vaping|Nicotine Dependence
December 18, 2020Phase 4
NCT03235505University of Oulu|Lapland Central Hospital Rovaniemi Finland
Smoking Cessation|Electronic Cigarette
August 1, 2018Phase 4
NCT02681510University of Wisconsin, Madison
Smoking
February 2016Phase 4
Molecular Weight

361.35

Formula

C17H19N3O6
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(O)[C@H](O)[C@@H](O)C(O)=O.C1(C2CC3CNC2)=C3C=C(N=CC=N4)C4=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 20 mg/mL (55.35 mM; ultrasonic and warming and heat to 60°C)

DMSO : 14.29 mg/mL (39.55 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 2.7674 mL 13.8370 mL 27.6740 mL
5 mM 0.5535 mL 2.7674 mL 5.5348 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 (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.

  • 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: ≥ 1.43 mg/mL (3.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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: ≥ 1.43 mg/mL (3.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 10 mg/mL (27.67 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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.
Purity & Documentation

Purity: 99.96%

Data Sheet (277 KB) SDS (596 KB)

COA (246 KB)

Handling Instructions (2659 KB)
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 (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
DMSO / H2O 1 mM 2.7674 mL 13.8370 mL 27.6740 mL 69.1850 mL
5 mM 0.5535 mL 2.7674 mL 5.5348 mL 13.8370 mL
10 mM 0.2767 mL 1.3837 mL 2.7674 mL 6.9185 mL
15 mM 0.1845 mL 0.9225 mL 1.8449 mL 4.6123 mL
20 mM 0.1384 mL 0.6918 mL 1.3837 mL 3.4592 mL
25 mM 0.1107 mL 0.5535 mL 1.1070 mL 2.7674 mL
30 mM 0.0922 mL 0.4612 mL 0.9225 mL 2.3062 mL
H2O 40 mM 0.0692 mL 0.3459 mL 0.6918 mL 1.7296 mL
50 mM 0.0553 mL 0.2767 mL 0.5535 mL 1.3837 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.

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Varenicline Tartrate Related Classifications

Keywords:

Varenicline375815-87-5CP 526555-18nAChRERKp38 MAPKNicotinic acetylcholine receptorsExtracellular signal regulated kinasessmoking cessationpartial agonistnicotineHUVECInhibitorinhibitorinhibit

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