| Field | Specification |
|---|---|
| Alternative names | CP 526555 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C13H13N3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Varenicline, also known as CP 526555, is an orally active partial agonist at the α4β2 nicotinic acetylcholine receptor (α4β2 nAChR), the principal mediator of nicotine dependence, with an IC50 of 250 nM. The compound also acts as a partial agonist at α6β2 nAChR and a full agonist at α7β2 nAChR. It blocks the direct agonist effects of nicotine on nAChR while itself stimulating nAChR in a more moderate way, and it has been widely used as an aid to smoking cessation[1][2][3][4][5]. It is supplied as a light yellow to yellow solid (C13H13N3, MW 211.27) at 99.92% purity.
Physical & Chemical Properties
| CAS Number | 249296-44-4 |
|---|---|
| Molecular Formula | C13H13N3 |
| Molecular Weight | 211.27 g/mol |
| Purity | 99.92% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | C12=C(C=C3N=CC=NC3=C2)C4CC1CNC4 |
| Signaling Pathway | Membrane Transporter/Ion Channel; Neuronal Signaling |
| Solubility | In Vitro: H2O: ≥ 20 mg/mL (94.67 mM) DMSO: 20 mg/mL (94.67 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
EC50: 2.3 μM (α4β2 nAChR); 18 μM (α7 nAChR); 55 μM (α3β4 nAChR)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| H2O | ≥ 20 mg/mL (94.67 mM) | — |
| DMSO | 20 mg/mL (94.67 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (11.83 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (11.83 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (11.83 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Varenicline (200 μM, 24 h) has no effect on the viability of HUVEC cells[3]. Varenicline (100 μM, 24 h) lowers VE-cadherin expression in HUVEC cells, while significant activation of ERK1/2 and p38 signaling occurs with Varenicline (100 μM, 30 min)[3]. Varenicline (100 μM, 4 h) increases HUVEC cell migration by 2.4-fold[3].
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
In rats, Varenicline (0.5, 1mg/kg, s.c., acute administration) reverses Fentanyl-induced respiratory depression in a dose-dependent manner and slightly alleviates Fentanyl-induced sedation[4]. In adult rhesus monkeys experienced with cocaine and nicotine, nicotine self-administration alone (0.0032 mg/kg/inj) and combined with cocaine (0.0032 mg/kg/inj) is dose-dependently reduced by Varenicline (0.004–0.04 mg/kg/h, i.v.drip, 23h a day for 7-10 d), with no significant effects on food-maintained responding[5]. In C57BL/6J and CD-1 mice, Varenicline (0.178-5.6 mg/kg, i.p., acute administration) displays antidepressant-like activity in the forced swim test[6].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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