2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. PHA-543613 dihydrochloride

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，Ki 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。

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PHA-543613 dihydrochloride Chemical Structure

PHA-543613 dihydrochloride Chemical Structure

CAS No. : 478148-58-2

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PHA-543613 dihydrochloride 的其他形式现货产品:

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PHA-543613 dihydrochloride 相关抗体

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  • 生物活性

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生物活性

PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value 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].

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

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
性状

固体

颜色

White to off-white

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)

纯度 & 产品资料
参考文献

PHA-543613 dihydrochloride 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

PHA-543613478148-58-2PHA543613PHA 543613nAChRNicotinic acetylcholine receptorsOrally activebrain penetrantAlzheimer's diseaseschizophreniaInhibitorinhibitorinhibit

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PHA-543613 dihydrochloride
目录号：
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