1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. nAChR
  3. Varenicline

Varenicline  (Synonyms: CP 526555)

Cat. No.: HY-10019 Purity: 99.98%
COA Handling Instructions

Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively. Varenicline is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment.

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

Varenicline Chemical Structure

Varenicline Chemical Structure

CAS No. : 249296-44-4

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 92 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
25 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 360 In-stock
Estimated Time of Arrival: December 31
100 mg USD 600 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of Varenicline:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[2]. Varenicline is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment[5].

IC50 & Target

EC50: 2.3 μM (α4β2 nAChR); 18 μM (α7 nAChR); 55 μM (α3β4 nAChR)[1]

In Vitro

Varenicline (1 μM, 24 h ) inhibits LPS-Induced cytokine secretions (IL-1β, IL-6, and TNF α) and cell proliferation rate in RAW 264.7 macrophages[1].
Varenicline (250 nM) evokes action potentials (Aps) in the absence of ACh stimulation in Human adrenal chromaffin cells isolated from male and female organ donors[3].
Varenicline (100 μM, 4 h) promotes migration of HUVECs by lowering the protein expression of VE-cadherin[4].

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

Cell Proliferation Assay[1]

Cell Line: RAW 264.7 murine macrophage cells (treated with 4 μg/mL LPS for 24 h)
Concentration: 1 μM
Incubation Time: 0-48 h
Result: Decreased the LPS-induced cell proliferation rate.

Western Blot Analysis[4]

Cell Line: HUVECs
Concentration: 1, 10, 100 μM
Incubation Time: 24 h or 30 min
Result: Decreased the protein expression of VE-cadherin and activated ERK1/2, p38 and JNK signaling.
In Vivo

Varenicline (Subcutaneous injection, 0.01-1 mg/kg, 3 days) given 10 min prior to nicotine (0.5 mg/kg, s.c.) inhibits nicotine conditioned place preference (CPP)[5].
Varenicline (Subcutaneous injection, 2.5 mg/kg, 3 days) results in a place aversion which is dependent on α5 nAChRs but not β2 nAChRs[5].
Varenicline (Subcutaneous injection, 0.1 and 0.5 mg/kg, 3 days) reverses nicotine withdrawal signs such as hyperalgesia and somatic signs and withdrawal-induced aversion in a dose-related manner[5].

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

Animal Model: ICR male mice[5]
Dosage: 0.01-1 mg/kg for 3 days
Administration: Subcutaneous injection
Result: Inhibited nicotine conditioned place preference (CPP) in a dose dependent manner.
Clinical Trial
Molecular Weight

211.26

Formula

C13H13N3

CAS No.
SMILES

C12=C(C=C3N=CC=NC3=C2)C4CC1CNC4

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 25 mg/mL (118.34 mM; Need ultrasonic)

H2O : ≥ 20 mg/mL (94.67 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.7335 mL 23.6675 mL 47.3350 mL
5 mM 0.9467 mL 4.7335 mL 9.4670 mL
10 mM 0.4734 mL 2.3668 mL 4.7335 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (11.83 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (11.83 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (11.83 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
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.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Varenicline
Cat. No.:
HY-10019
Quantity:
MCE Japan Authorized Agent: