Varenicline (Tartrate)


CAS No. : 375815-87-5

(Synonyms: CP 526555-18)

375815-87-5
Price and Availability of CAS No. : 375815-87-5
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
We match the lowest price on market.

We offer a substantial discount on larger orders, please inquire via [email protected]

or Fax: (86)21-58955996

Inquiry for price and availability only. Please place your order via our email or fax.

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)
Introduction of 375815-87-5 :

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].

Your information is safe with us.