1240514-89-9

1240514-89-9 structure

Name: VU0364572 TFA salt
Chemical Name: Ethyl (3R)-3-[(2-methylbenzoyl)amino]-1,4'-bipiperidine-1'-carboxylate trifluoroacetate (1:1)
CAS Number: 1240514-89-9
Molecular Formula: C₂₃H₃₂F₃N₃O₅
Molecular Weight: 487.51
Create Date: 2018-06-28 16:06:08
Modify Date: 2024-01-10 12:09:28
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].

Name	Ethyl (3R)-3-[(2-methylbenzoyl)amino]-1,4'-bipiperidine-1'-carboxylate trifluoroacetate (1:1)
Synonyms	Ethyl (3R)-3-[(2-methylbenzoyl)amino]-1,4'-bipiperidine-1'-carboxylate trifluoroacetate (1:1) [1,4'-Bipiperidine]-1'-carboxylic acid, 3-[(2-methylbenzoyl)amino]-, ethyl ester, (3R)-, compd. with 2,2,2-trifluoroacetic acid (1:1)

Description	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].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> mAChR Signaling Pathways >> GPCR/G Protein >> mAChR Research Areas >> Neurological Disease
Target	mAChR1:0.11 μM (EC50)
In Vitro	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: 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.
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: 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.
References	[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.

Molecular Formula	C₂₃H₃₂F₃N₃O₅
Molecular Weight	487.51
Exact Mass	487.229401

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