2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. nAChR 5-HT Receptor
  4. A-582941 dihydrochloride

A-582941 dihydrochloride 

目录号: HY-59201A 纯度: 99.78%
COA 产品使用指南

摩尔计算器

A-582941 dihydrochloride 是一种有效的，选择性的和可透过血脑屏障的 α7 nAChR 的部分激动剂，在大鼠脑膜和人额叶皮层的 Ki 值分别为 10.8 nM 和 16.7 nM。A-582941 dihydrochloride 以 150 nM 的 Ki 值与人 5-HT3 受体结合。A-582941 dihydrochloride 具有研究与各种神经退行性疾病和精神疾病相关的认知缺陷的潜力。

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A-582941 dihydrochloride Chemical Structure

A-582941 dihydrochloride Chemical Structure

CAS No. : 848591-90-2

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Customer Review

A-582941 dihydrochloride 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research[1][2].

IC50 & Target[1]

α7 nAChR

10.8 nM (Ki, for rat α7 receptors)

α7 nAChR

16.7 nM (Ki, for human α7 receptors)

5-HT3 Receptor

150 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
> 100 μM
Compound: 32
Agonist activity at human recombinant alpha4beta2 nicotinic acetylcholine receptor expressed in HEK293 cells assessed as changes in intracellular calcium level by FLIPR
Agonist activity at human recombinant alpha4beta2 nicotinic acetylcholine receptor expressed in HEK293 cells assessed as changes in intracellular calcium level by FLIPR
[PMID: 19552432]
Oocyte EC50
4.26 μM
Compound: 32
Agonist activity at human recombinant alpha7 nicotinic acetylcholine receptor expressed in xenopus laevis oocytes by parallel oocyte electrophysiological assay
Agonist activity at human recombinant alpha7 nicotinic acetylcholine receptor expressed in xenopus laevis oocytes by parallel oocyte electrophysiological assay
[PMID: 19552432]
体外研究
(In Vitro)

A-582941 (0.1-100 μM) protects against cell death induced by NGF withdrawal in PC12 cells[2].
A-582941 (100 nM) increases the number of inhibitory postsynaptic potentials (IPSCs) by 260±70%, the sum of amplitudes by 220±30%, and the sum of areas by 210±40%[2].
A-582941 increases ERK1/2 phosphorylation with an EC50 of 95 nM in PC12 cells[2].

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

A-582941 dihydrochloride 相关抗体:
体内研究
(In Vivo)

A-582941 (3 μM/kg, i.p. once daily for 3 d) induces a moderate increase in ACh release in the medial prefrontal cortex (mPFCx) of freely moving rats[2].
A-582941 (0.01-1.00 μM/kg, i.p.) produces a dose-dependent increase in ERK1/2 phosphorylation in the cingulate cortex and hippocampus, and increases cAMP response element-binding protein (CREB) phosphorylation in the cingulate cortex in mice[2].
A-582941 (0.1-1.0 μM/kg, i.p.) evokes dose-dependent increases in Ser-9 GSK-3β phosphorylation in the mouse cingulate cortex[2].
A-582941 shows high oral bioavailability (mouse ~100%, rat 90%, dog 22%, monkey 50%) and Cmax (mouse 18, rat 114, dog 79, monkey 39 ng/mL) following oral administration (mouse 1.0, rat 6.2, dog 3.0, monkey 3.0 μM/kg)[2].
A-582941 shows terminal elimination half-lives (mouse 1.4, rat 1.5, dog 1.4, monkey 2.0 h), plasma clearance (mouse 7.9, rat 4.7, dog 5.3, monkey 1.6 L/h/kg) and volumes of distribution (mouse 11.4, rat 9.2, dog 7.9, monkey 3.9 L/kg) following intravenous administration (mouse 1.0, rat 6.2, dog 0.5, monkey 0.5 μM/kg)[2].

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

Animal Model: Male Sprague-Dawley CD rats (250-275 g)[2]
Dosage: 3 μM/kg
Administration: I.p. once daily for 3 days
Result: Increased the releases of Ach.
The effect remained stable after the second and third administration.
分子量

353.29

Formula

C17H22Cl2N4
CAS 号
性状

固体

颜色

Light yellow to 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 : 100 mg/mL (283.05 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 2.8305 mL 14.1527 mL 28.3054 mL
5 mM 0.5661 mL 2.8305 mL 5.6611 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

只
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

纯度: 99.78%

COA (261 KB) HNMR (259 KB) LCMS (93 KB)

产品使用指南 (1538 KB)
参考文献

A-582941 dihydrochloride 相关分类

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 2.8305 mL 14.1527 mL 28.3054 mL 70.7634 mL
5 mM 0.5661 mL 2.8305 mL 5.6611 mL 14.1527 mL
10 mM 0.2831 mL 1.4153 mL 2.8305 mL 7.0763 mL
15 mM 0.1887 mL 0.9435 mL 1.8870 mL 4.7176 mL
20 mM 0.1415 mL 0.7076 mL 1.4153 mL 3.5382 mL
25 mM 0.1132 mL 0.5661 mL 1.1322 mL 2.8305 mL
30 mM 0.0944 mL 0.4718 mL 0.9435 mL 2.3588 mL
40 mM 0.0708 mL 0.3538 mL 0.7076 mL 1.7691 mL
50 mM 0.0566 mL 0.2831 mL 0.5661 mL 1.4153 mL
60 mM 0.0472 mL 0.2359 mL 0.4718 mL 1.1794 mL
80 mM 0.0354 mL 0.1769 mL 0.3538 mL 0.8845 mL
100 mM 0.0283 mL 0.1415 mL 0.2831 mL 0.7076 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.

Keywords:

A-582941848591-90-2A582941A 582941nAChR5-HT ReceptorNicotinic acetylcholine receptorsSerotonin Receptor5-hydroxytryptamine Receptorpartialα75-HT3cognitivedeficitsneurodegenerativepsychiatricInhibitorinhibitorinhibit

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