Cerlapirdine free base

Cerlapirdine, also known as SAM-531, WAY-262, 531 and PF-05212365, is a selective, potent, full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has been in clinical development for the treatment of cognitive disorders associated with Alzheimer's disease and schizophrenia. As of 2011, it is in phase II clinical trials, and has demonstrated a trend toward efficacy along with a good side effect profile and no incidence of serious adverse events. It exerts its effects by acting as a selective 5-HT6 receptor antagonist.

Product information

CAS Number: 925448-93-7

Molecular Weight: 409.50

Formula: C22H23N3O3S

Synonym:

SAM531

PF-05212365

Chemical Name: N, N-dimethyl-3-[(3-naphthalen-1-ylsulfonyl-2H-indazol-5-yl)oxy]propan-1-amine

Smiles: CN(C)CCCOC1=CC2=C(NN=C2C=C1)S(=O)(=O)C1=CC=CC2=CC=CC=C21

InChiKey: NXQGEDVQXVTCDA-UHFFFAOYSA-N

InChi: InChI=1S/C22H23N3O3S/c1-25(2)13-6-14-28-17-11-12-20-19(15-17)22(24-23-20)29(26,27)21-10-5-8-16-7-3-4-9-18(16)21/h3-5,7-12,15H,6,13-14H2,1-2H3,(H,23,24)

Technical Data

Appearance: Solid Power

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

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Tse S, Leung L, Raje S, Seymour M, Shishikura Y, Obach RS. Disposition and metabolic profiling of [(14)C]cerlapirdine using accelerator mass spectrometry. Drug Metab Dispos. 2014 Dec;42(12):2023-32. doi: 10.1124/dmd.114.059675. Epub 2014 Sep 12. PubMed PMID: 25217486.
2. Ly S, Pishdari B, Lok LL, Hajos M, Kocsis B. Activation of 5-HT6 receptors modulates sleep-wake activity and hippocampal theta oscillation. ACS Chem Neurosci. 2013 Jan 16;4(1):191-9. doi: 10.1021/cn300184t. Epub 2012 Dec 10. PubMed PMID: 23336058; PubMed Central PMCID: PMC3547479.
3. Macauley D. American Chemical Society-239th national meeting--Investigating new therapeutic candidates: part 1. 21-25 March 2010, San Francisco, CA, USA. IDrugs. 2010 May;13(5):289-91. PubMed PMID: 20432180.

Products are for research use only. Not for human use.