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VU0456940

Catalog No. T35080 CAS T35080

Synonyms: VU-0456940, VU 0456940

VU0456940 is a potent M1 PAM with excellent selectivity (hM1 EC50 = 340 nM, 14-fold leftward shift of the ACh CRC; hM2–hM5 inactive). VU0456940 potentiated the excitation of a subthreshold concentration of CCh in MSNs. VU0456940 shifted APP processing and engaged the nonamyloidogenic pathway inducing the release of sAPPα in the presence of a 100 nm CCh dose (displayed no activity in the absence of CCh).

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VU0456940, CAS T35080

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Biological Description

Chemical Properties

Storage & Solubility Information

Description

Synonyms	VU-0456940, VU 0456940
Molecular Weight	511.5
Formula	C24H19F2N5O4S
CAS No.	T35080

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Tarr JC, et al. Targeting selective activation of M1 for the treatment of Alzheimer’s disease: further chemical optimization and pharmacological characterization of the M1 positive allosteric modulator ML169. ACS Chem. Neurosci. 2012;3:884–895. 2. Reid PR, et al. Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN Probe. Bioorg. Med. Chem. Lett. 2011;21:2697–2701. 3. Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects Jennifer E. Davoren, Che-Wah Lee, Michelle Garnsey, , and Sarah Grimwood Publication Date (Web): June 8, 2016 (Article) DOI: 10.1021/acs.jmedchem.6b00544

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

VU0456940 T35080 VU-0456940 VU 0456940 inhibitor inhibit

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