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

Varenicline Hydrochloride (Synonyms: CP 526555 hydrochloride)

Cat. No.: HY-10020 Purity: 98.87%
Handling Instructions

Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a Ki value of 0.12 nM.

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

Varenicline Hydrochloride Chemical Structure

Varenicline Hydrochloride Chemical Structure

CAS No. : 230615-23-3

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10 mM * 1 mL in DMSO USD 92 In-stock
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Description

Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist[1][2][3]. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a Ki value of 0.12 nM[4].

IC50 & Target

nAChR[1]

In Vivo

Varenicline (0.5-2 mg/kg/day; subcutaneous injection; twice daily; for 14 days; male Wistar rats) treatment shows a comparable significantly higher DRD2/3 availability in the ventral striatum of approximately 11%, while only the rats treated with 1 and 2 mg/kg/day dose shows significantly higher DRD2/3 availability in the dorsal striatum by 12.5% and 13.2%, respectively. Varenicline induces dose-dependent and sustained increases in striatal DRD2/3 in rats, particularly in the ventral striatum[1].

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

Animal Model: Eighty male Wistar rats (250-300 g)[1]
Dosage: 0.5 mg/kg/day, 1 mg/kg/day or 2 mg/kg/day
Administration: Subcutaneous injection; twice daily; for 14 days
Result: Significantly higher DRD2/3 availability in the ventral striatum of approximately 11%, while only the rats treated with 1 and 2 mg/kg/day dose showed significantly higher DRD2/3 availability in the dorsal striatum by 12.5% and 13.2%, respectively.
Clinical Trial
Molecular Weight

247.72

Formula

C₁₃H₁₄ClN₃

CAS No.
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: 

H2O : 50 mg/mL (201.84 mM; Need ultrasonic)

DMSO : ≥ 2.5 mg/mL (10.09 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0368 mL 20.1841 mL 40.3682 mL
5 mM 0.8074 mL 4.0368 mL 8.0736 mL
10 mM 0.4037 mL 2.0184 mL 4.0368 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Varenicline Hydrochloride
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HY-10020
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