A-582941 dihydrochloride|cas:848591-90-2|西域试剂

A-582941 dihydrochloride,98.64%

产品编号：Bellancom-59201A| CAS NO：848591-90-2| 分子式：C₁₇H₂₂Cl₂N₄| 分子量：353.29

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货号	价格	库存与货期
Bellancom-59201A	￥1500.00	杭州北京（现货）
Bellancom-59201A	￥2500.00	杭州北京（现货）
Bellancom-59201A	￥5500.00	杭州北京（现货）
Bellancom-59201A	￥9500.00	杭州北京（现货）

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A-582941 dihydrochloride

产品介绍

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 K_i 值分别为 10.8 nM 和 16.7 nM。A-582941 dihydrochloride 以 150 nM 的 K_i 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。

生物活性

A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with K_is 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 K_i of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research.

体外研究

A-582941 (0.1-100 μM) protects against cell death induced by NGF withdrawal in PC12 cells.
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%.
A‐582941 increases ERK1/2 phosphorylation with an EC₅₀ of 95 nM in PC12 cells.

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

体内研究

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.
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.
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.
A‐582941 shows high oral bioavailability (mouse ~100%, rat 90%, dog 22%, monkey 50%) and C_max (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).
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).

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

Animal Model:	Male Sprague-Dawley CD rats (250-275 g)
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.

体内研究

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

Animal Model:	Male Sprague-Dawley CD rats (250-275 g)
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (283.05 mM; Need ultrasonic)

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
10 mM	0.2831 mL	1.4153 mL	2.8305 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°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。

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)

参考文献