PHA-543613 dihydrochloride

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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。

CAS NO:

478148-58-2

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

PHA-543613 dihydrochloride 是一种有效的、具有口服活性、可穿过血脑屏障和选择性的α7 nAChR激动剂，K_i为 8.8 nM。PHA-543613 dihydrochloride 对 α7-nAChR 的选择性优于 α3β4、α1β1γδ、α4β2 和 5-HT3 受体。PHA-543613 dihydrochloride 可用于阿尔茨海默病和精神分裂症的认知缺陷研究。

生物活性

PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selectiveα7nAChRagonist with aK_ivalue of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors^[1]. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research^[2]^[3].

IC₅₀& Target

Ki: 8.8 nM (α7 nAChR)^[1]

体内研究
(In Vivo)

PHA-543613 dihydrochloride (0.3 mg/kg) successfully reverses Scopolamine-induced short-term memory deficits in rats^[2].
PHA-543613 dihydrochloride (4 and 12 mg/kg; i.p. once) reduces behavioral deficits and brain edema is dependent on the PI3K-Akt signaling pathway^[3].

Animal Model:	Male CD-1 mice with (intracerebral hemorrhage) ICH-induction or sham surgery^[3]
Dosage:	4 and 12 mg/kg
Administration:	Intraperitoneal injection; 4 and 12 mg/kg; 1 hour after surgery
Result:	Increased p-Akt and decreased p-GSK-3 and CC3 expressions in the ipsilateral hemisphere and reduced the neuronal cell death in the perihematomal area. Attenuated behavioral deficits and brain edema at 72 hours after ICH.

分子量

344.24

Formula

C₁₅H₁₉Cl₂N₃O₂

CAS 号

478148-58-2

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.