VU0456940
| Code | Size | Price |
|---|
| TAR-T35080-100mg | 100mg | Enquire | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T35080-500mg | 500mg | Enquire | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20°C
Documents
Further Information
Bioactivity:
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).
CAS:
T35080
Molecular Weight:
511.5
Purity:
0.98
SMILES:
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
References
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.
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
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.