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A-582941 dihydrochloride
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。
A-582941 dihydrochloride图片
CAS NO:848591-90-2
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

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。
生物活性

A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist ofα7nAChR, withKis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human5-HT3receptorwith aKiof 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research[1][2].

IC50& Target[1]

5-HT3Receptor

150 nM (Ki)

α7 nAChR

10.8 nM (Ki, for rat α7 receptors)

α7 nAChR

16.7 nM (Ki, for human α7 receptors)

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 EC50of 95 nM in PC12 cells[2].

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‐inding 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].

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

848591-90-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.