Varenicline B

Research use only, not for human use.

Varenicline (CP 526555) is a selective partial agonist of the α4β2 nAChR and a full agonist of the α3β4 nAChR and α7 nAChR to help smokers with cardiovascular disease and COPD quit smoking.

Varenicline (CP 526555) 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.

Cell Viability AssayCell Line:HUVEC Concentration:100, 200, 300, 500 μMIncubation Time:24 hResult: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 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 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.

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Cell Cycle/DNA Damage

AChR

AChR

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249296-44-4

211.26

C13H13N3

>98% (HPLC)

In Vitro:?DMSO : 20 mg/mL (94.67 mM; Ultrasonic )H2O : ≥ 20 mg/mL (94.67 mM)

N1=CC=NC2=CC3=C(C=C12)C4CNCC3C4

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(-20℃)

With Ice Pack

≥ 2 years