PZ0394
PF-05212377 succinate
≥98% (HPLC)
Synonym(s):
2-Methyl-1-(phenylsulfonyl)-4-piperazin-1-yl-1H-benzimidazole, succinate salt, PF 05212377 succinate, PF 5212377 succinate, PF-5212377 succinate, PF05212377 succinate, PF5212377 succinate, SAM-760 succinate, WYE-103760 succinate
Sign Into View Organizational & Contract Pricing
Select a Size
About This Item
Empirical Formula (Hill Notation):
C18H20N4O2S · xC4H6O4
Molecular Weight:
356.44 (free base basis)
UNSPSC Code:
12352202
NACRES:
NA.77
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
room temp
Biochem/physiol Actions
PF-05212377 (SAM-760; WYE-103760) is an orally available, high-affinity, selective 5-hydroxytryptamine (5-HT; serotonin) receptor 5-HT6 antagonist (Ki/IC50 = 0.53/1.06 nM against 3 nM [3H]-LSD for binding human 5-HT6). PF-05212377 modulates glutamate and acetylcholine release in the cerebral cortex and hippocampus in rodents with in vivo pro-cognitive efficacy.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
This item has
Choose from one of the most recent versions:
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
Terence Fullerton et al.
Alzheimer's research & therapy, 10(1), 38-38 (2018-04-07)
Symptomatic benefits have been reported for 5-HT6 receptor antagonists in Alzheimer's disease (AD) trials. SAM-760 is a potent and selective 5-HT6 receptor antagonist that has demonstrated central 5-HT6 receptor saturation in humans at a dose of 30 mg. This was
Aarti Sawant-Basak et al.
Drug metabolism and disposition: the biological fate of chemicals, 46(7), 934-942 (2018-04-27)
SAM-760 [(2-methyl-1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-benzo[d]imidazole)], a 5HT6 antagonist, was investigated in humans for the treatment of Alzheimer's disease. In liver microsomes and recombinant cytochrome P450 (P450) isozymes, SAM-760 was predominantly metabolized by CYP3A (∼85%). Based on these observations and an expectation of a
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
Contact Technical Service