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

Varenicline dihydrochloride  (Synonyms: CP 526555 dihydrochloride)

Cat. No.: HY-10019A Purity: 99.21%
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Varenicline (CP 526555-18) 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.

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

Varenicline dihydrochloride Chemical Structure

Varenicline dihydrochloride Chemical Structure

CAS No. : 866823-63-4

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10 mg USD 90 In-stock
25 mg USD 180 In-stock
50 mg USD 270 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Varenicline dihydrochloride:

Varenicline dihydrochloride Related Antibodies

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Description

Varenicline (CP 526555-18) 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

EC50: 2.3 μM (α4β2 nAChR); 18 μM (α7 nAChR); 55 μM (α3β4 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 dihydrochloride 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, 200, 300, 500 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
Molecular Weight

284.18

Formula

C13H15Cl2N3
CAS No.
Appearance

Solid

Color

Brown to dark brown

SMILES

[H]Cl.[H]Cl.C1(C2)CNCC2C3=CC4=NC=CN=C4C=C13
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (351.89 mM)

DMSO : 62.5 mg/mL (219.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5189 mL 17.5945 mL 35.1890 mL
5 mM 0.7038 mL 3.5189 mL 7.0378 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 and light). 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation
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 and light). 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 3.5189 mL 17.5945 mL 35.1890 mL 87.9724 mL
5 mM 0.7038 mL 3.5189 mL 7.0378 mL 17.5945 mL
10 mM 0.3519 mL 1.7594 mL 3.5189 mL 8.7972 mL
15 mM 0.2346 mL 1.1730 mL 2.3459 mL 5.8648 mL
20 mM 0.1759 mL 0.8797 mL 1.7594 mL 4.3986 mL
25 mM 0.1408 mL 0.7038 mL 1.4076 mL 3.5189 mL
30 mM 0.1173 mL 0.5865 mL 1.1730 mL 2.9324 mL
40 mM 0.0880 mL 0.4399 mL 0.8797 mL 2.1993 mL
50 mM 0.0704 mL 0.3519 mL 0.7038 mL 1.7594 mL
60 mM 0.0586 mL 0.2932 mL 0.5865 mL 1.4662 mL
80 mM 0.0440 mL 0.2199 mL 0.4399 mL 1.0997 mL
100 mM 0.0352 mL 0.1759 mL 0.3519 mL 0.8797 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 dihydrochloride Related Classifications

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  • 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.

Keywords:

Varenicline866823-63-4CP 526555CP526555CP-526555nAChRNicotinic acetylcholine receptorssmoking cessationpartial agonistnicotineHUVECInhibitorinhibitorinhibit

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