PHA-543613

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PHA-543613

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:

478149-53-0

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品介绍

PHA-543613 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 对 α7-nAChR 的选择性优于 α3β4、α1β1γδ、α4β2 和 5-HT3 受体。PHA-543613 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 is a potent, orally active, brain-penetrant and selectiveα7nAChRagonist with aK_iof 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors^[1]. PHA-543613 can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research^[2].

IC₅₀& Target

Ki: 8.8 nM (α7 nAChR)^[1]

体内研究
(In Vivo)

PHA-543613 (0.3 mg/kg) successfully reverses Scopolamine-induced short-term memory deficits in rats^[2].
PHA-543613 (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

271.31

性状

Solid

Formula

C₁₅H₁₇N₃O₂

CAS 号

478149-53-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 250 mg/mL(921.46 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.6858 mL	18.4291 mL	36.8582 mL
5 mM	0.7372 mL	3.6858 mL	7.3716 mL
10 mM	0.3686 mL	1.8429 mL	3.6858 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。