WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 526731
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).
MedKoo Cat#: 526731
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
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
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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
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
The following data is based on the product molecular weight 511.5038 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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