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SUVN-911
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SUVN-911图片
CAS NO:2414674-71-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
SUVN-911 是一种高效、选择性的,有大脑通透性和口服生物活性的神经元烟碱乙酰胆碱 α4β2 受体 (α4β2 receptor) 拮抗剂,Ki值为 1.5 nM。SUVN-911 具有抗抑郁作用。
生物活性

SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholineα4β2 receptorantagonist, with aKiof 1.5 nM. SUVN-911 has antidepressant activity[1].

IC50& Target

Ki: 1.5 nM (α4β2 receptor)[1]

体外研究
(In Vitro)

SUVN-911 displays high selectivity for α4β2 over α3β4 nAChR[1].
SUVN-911 shows good selectivity against over 70 receptors which includes GPCRs, ion channels, enzymes, peptides, steroids, second messengers, growth factors and prostaglandins[1].

体内研究
(In Vivo)

SUVN-911 is devoid of cardiovascular and gastrointestinal side effects[1].
SUVN-911 (1.0-10.0 mg/kg; p.o.; daily; for 3 days) shows significant antidepressant effects[1].
SUVN-911 shows metabolic stability in rats[1].
SUVN-911 (3 mg/kg; p.o.) has shown high oral exposures, longer half-lives and adequate brain penetration in Wistar rats[1].

Animal Model:Male Wistar rats (180-230 g)[1]
Dosage:1 mg/kg, 3 mg/kg, 10.0 mg/kg
Administration:Oral administration, daily, for 3 days
Result:Showed antidepressant like activity with no signs of tachyphylaxis.
Animal Model:Male Wistar rats (225 ± 25 g)[1]
Dosage:3 mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration
Result:AUC=3507 ng*h/mL, T1/2=3.34 hours.
Clinical Trial
分子量

261.15

性状

Solid

Formula

C11H14Cl2N2O

CAS 号

2414674-71-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 125 mg/mL(478.65 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.8292 mL19.1461 mL38.2922 mL
5 mM0.7658 mL3.8292 mL7.6584 mL
10 mM0.3829 mL1.9146 mL3.8292 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。