VU0364572 TFA_product_DataBase

Bioactivity	VU0364572 TFA is a 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 orally active and is CNS penetrant[1][3].
Invitro	VU0364572 (30 μM; 25 min) TFA 促进 striatal/NAc 切片中 KCNQ2、NR1 和 MARCKS 的磷酸化[2]。 Western Blot Analysis[2] Cell Line:
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]。 Animal Model:
Name	VU0364572 TFA
CAS	1240514-89-9
Formula	C23H32F3N3O5
Molar Mass	487.51
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

PeptideDB