Varenicline B

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Varenicline (CP 526555) 是具有口服活性的尼古丁依赖主要介质 α4β2 烟碱型乙酰胆碱受体 (α4β2 nAChR) 的部分激动剂 (IC50 = 250 nM)。Varenicline 也是 α6β2 nAChR 的部分激动剂和 α6β2 nAChR 的完全激动剂。 Varenicline 可阻断尼古丁对 nAChR 的直接激动作用，同时以更温和的程度刺激 nAChR，被广泛用作戒烟的辅助手段。

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 中的溶解度 : 20 mg/mL (94.67 mM; 超声助溶 ) H2O 中的溶解度 : ≥ 20 mg/mL (94.67 mM)

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

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(-20℃)

With Ice Pack

≥ 2 years