1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. nAChR
  3. SUVN-911

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。

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SUVN-911 Chemical Structure

SUVN-911 Chemical Structure

CAS No. : 2414674-71-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2858
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1 mg ¥995
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5 mg ¥2850
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10 mg ¥4300
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Customer Review

Other Forms of SUVN-911:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity[1].

IC50 & Target

Ki: 1.5 nM (α4β2 receptor)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 10 μM
Compound: 9h; SUVN-911
Inhibition of recombinant human ERG expressed in HEK293 at -80 mV holding potential by whole-cell patch clamp method
Inhibition of recombinant human ERG expressed in HEK293 at -80 mV holding potential by whole-cell patch clamp method
[PMID: 32026697]
HEK293 IC50
7.31 μM
Compound: 9h; SUVN-911
Antagonist activity at alpha4beta2 nAChR (unknown origin) expressed in HEK293 cells assessed as reduction in acetylcholine-induced currents at -80 mV holding potential by whole-cell patch clamp method
Antagonist activity at alpha4beta2 nAChR (unknown origin) expressed in HEK293 cells assessed as reduction in acetylcholine-induced currents at -80 mV holding potential by whole-cell patch clamp method
[PMID: 32026697]
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C11H14Cl2N2O

CAS 号
性状

固体

颜色

Off-white to light yellow

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
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (478.65 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.8292 mL 19.1461 mL 38.2922 mL
5 mM 0.7658 mL 3.8292 mL 7.6584 mL
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8292 mL 19.1461 mL 38.2922 mL 95.7304 mL
5 mM 0.7658 mL 3.8292 mL 7.6584 mL 19.1461 mL
10 mM 0.3829 mL 1.9146 mL 3.8292 mL 9.5730 mL
15 mM 0.2553 mL 1.2764 mL 2.5528 mL 6.3820 mL
20 mM 0.1915 mL 0.9573 mL 1.9146 mL 4.7865 mL
25 mM 0.1532 mL 0.7658 mL 1.5317 mL 3.8292 mL
30 mM 0.1276 mL 0.6382 mL 1.2764 mL 3.1910 mL
40 mM 0.0957 mL 0.4787 mL 0.9573 mL 2.3933 mL
50 mM 0.0766 mL 0.3829 mL 0.7658 mL 1.9146 mL
60 mM 0.0638 mL 0.3191 mL 0.6382 mL 1.5955 mL
80 mM 0.0479 mL 0.2393 mL 0.4787 mL 1.1966 mL
100 mM 0.0383 mL 0.1915 mL 0.3829 mL 0.9573 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
SUVN-911
目录号:
HY-136146
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