| 产品描述: | 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. |
| 靶点: |
mAChR1:0.11 μM (EC50) |
| 体外研究: |
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。 |
| 体内研究: |
VU0364572 (30 μM; 25 min) TFA 促进 striatal/NAc 切片中 KCNQ2、NR1 和 MARCKS 的磷酸化。 |
| 参考文献: |
1. Lebois EP, et al. Disease-Modifying Effects of M1 Muscarinic Acetylcholine Receptor Activation in an Alzheimer's Disease Mouse Model. ACS Chem Neurosci. 2017 Jun 21;8(6):1177-1187. 2. Faruk MO, et al. Muscarinic signaling regulates voltage-gated potassium channel KCNQ2 phosphorylation in the nucleus accumbens via protein kinase C for aversive learning. J Neurochem. 2022 Feb;160(3):325-341. 3. Lebois EP, et al. Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6451-5. |
| 保存条件: |
-80°C 12个月; -20°C 6个月,干燥, 避光 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.051 ml |
10.256 ml |
20.512 ml |
| 5 mM |
0.41 ml |
2.051 ml |
4.102 ml |
| 10 mM |
0.205 ml |
1.026 ml |
2.051 ml |
| 50 mM |
0.041 ml |
0.205 ml |
0.41 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |