2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. VU0364572 TFA

VU0364572 TFA 是一种具有口服活性和选择性的 M1 毒蕈碱受体 (M1 muscarinic receptor) 变构激动剂，EC50 为 0.11 μM。VU0364572 TFA 具有预防记忆障碍和减少阿尔茨海默病神经病理的神经保护潜力。VU0364572 TFA 对中枢神经系统具有渗透性。

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VU0364572 TFA Chemical Structure

VU0364572 TFA Chemical Structure

CAS No. : 1240514-89-9

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规格 价格 是否有货 数量
5 mg ￥5465
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VU0364572 TFA 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant[1][3].

IC50 & Target[3]

mAChR1

0.11 μM (EC50)

体外研究
(In Vitro)

VU0364572 (30 μM; 25 min) TFA 促进 striatal/NAc 切片中 KCNQ2、NR1 和 MARCKS 的磷酸化[2]。

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

VU0364572 TFA 相关抗体:

Western Blot Analysis[2]

Cell Line: Striatal/NAc slices
Concentration: 30 μM
Incubation Time: 25 min
Result: Significantly increased the phosphorylation of KCNQ2 at T217, NR1 at S890, and MARCKS at S152/156.
体内研究
(In Vivo)

VU0364572 TFA (10 mg/kg/day; oral; 4 months) TFA 在 5XFAD 转基因阿尔茨海默氏症小鼠中显示出神经保护作用。VU0364572 的半衰期为 45 分钟[1]。

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

Animal Model: 5XFAD transgenic Alzheimer’s mice[1]
Dosage: 10 mg/kg/day
Administration: In drinking water, from 2 months of age to 6 months
Result: Preserved hippocampal memory. Significantly reduced levels of soluble and insoluble Aβ40,42 in the cortex and hippocampus of these animals. Significantly decreased oligomeric (oAβ) levels in the cortex.
分子量

487.51

Formula

C23H32F3N3O5
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 and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

纯度 & 产品资料
参考文献

VU0364572 TFA 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VU03645721240514-89-9VU 0364572VU-0364572mAChRMuscarinic acetylcholine receptorAlzheimer’s DiseaseKCNQ2NR1MARCKSstriatal/NAc5XFADInhibitorinhibitorinhibit

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