VU0456940

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MedKoo CAT#: 526731

CAS#: Unknown

Description: 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).


Price and Availability

Size Price Shipping out time Quantity
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Pricing updated 2020-10-29. Prices are subject to change without notice.

VU-0456940 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 526731
Name: VU0456940
CAS#: Unknown
Chemical Formula: C24H19F2N5O4S
Exact Mass: 511.1126
Molecular Weight: 511.5038
Elemental Analysis: C, 56.36; H, 3.74; F, 7.43; N, 13.69; O, 12.51; S, 6.27


Synonym: VU-0456940, VU 0456940, VU0456940

IUPAC/Chemical Name: 1-[4,6-difluoro-1-[6-(1-methylpyrazol-4-yl)pyridin-3-yl]indol-3-yl]sulfonyl-3-(5-methyl-1,2-oxazol-3-yl)propan-2-one

InChi Key: WAZHEZAQAZUMHH-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H19F2N5O4S/c1-14-5-17(29-35-14)8-19(32)13-36(33,34)23-12-31(22-7-16(25)6-20(26)24(22)23)18-3-4-21(27-10-18)15-9-28-30(2)11-15/h3-7,9-12H,8,13H2,1-2H3

SMILES Code: CN1N=CC(C2=CC=C(N3C=C(S(=O)(CC(CC4=NOC(C)=C4)=O)=O)C5=C3C=C(F)C=C5F)C=N2)=C1


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


References

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, Michael A. Brodney, Jason Cordes, Keith Dlugolenski, Jeremy R. Edgerton, Anthony R. Harris, Christopher J. Helal, Stephen Jenkinson, Gregory W. Kauffman, Terrence P. Kenakin, John T. Lazzaro, Susan M. Lotarski, Yuxia Mao, Deane M. Nason, Carrie Northcott, Lisa Nottebaum, Steven V. O’Neil, Betty Pettersen, Michael Popiolek, Veronica Reinhart, Romelia Salomon-Ferrer, Stefanus J. Steyn, Damien Webb, Lei Zhang, and Sarah Grimwood Publication Date (Web): June 8, 2016 (Article) DOI: 10.1021/acs.jmedchem.6b00544