Size | Price | Stock |
---|---|---|
5mg | $84 | In-stock |
10mg | $120 | In-stock |
25mg | $228 | In-stock |
50mg | $360 | In-stock |
100mg | $600 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-10021 |
M.Wt: | 361.35 |
Formula: | C17H19N3O6 |
Purity: | >98 % |
Solubility: | DMSO : 14.29 mg/mL (ultrasonic);H2O : 20 mg/mL (ultrasonic;warming;heat to 60°C) |
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[1][2][3][4][5].
IC50 & Target:IC50: 250 nM (α4β2 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].
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].
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