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

Varenicline (Synonyms: CP 526555)

Cat. No.: HY-10019 Purity: 99.70%
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 cytisine, 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

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10 mM * 1 mL in DMSO USD 92 In-stock
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5 mg USD 84 In-stock
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10 mg USD 120 In-stock
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25 mg USD 228 In-stock
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50 mg USD 360 In-stock
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100 mg USD 600 In-stock
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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[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].

IC50 & Target

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

In Vivo

Varenicline (CP 526555) (subcutaneous injection; 0.01, 0.05, 0.1 and 1 mg/kg; 3 days) iven 10 min prior to nicotine, inhibits nicotine CPP in a dose dependent manner. At the doses of 0.1 and 1 mg/kg totally blocks the effect of nicotine in CPP test without inducing significant changes in preferences on their own[2].
Varenicline (2.5 mg/kg) results in a place aversion that was dependent on α5 nAChRs but not β2 nAChRs[2].
Varenicline (0.1 and 0.5 mg/kg) reverses nicotine withdrawal signs such as hyperalgesia and somatic signs and withdrawal-induced aversion in a dose-related manner[2].

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

Animal Model: ICR male mice (8 weeks)[1]
Dosage: 0.01, 0.05, 0.1 and 1 mg/kg
Administration: 3 days
Result: Supressed the effect of nicotine in CPP test.
Clinical Trial
Molecular Weight

211.26

Formula

C₁₃H₁₃N₃

CAS No.

249296-44-4

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)

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 provided by MCE.
References
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Keywords:

VareniclineCP 526555CP526555CP-526555nAChRNicotinic acetylcholine receptorsagonistsmokecessationCPPInhibitorinhibitorinhibit

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Varenicline
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