PZ0394
PF-05212377 succinate
≥98% (HPLC)
동의어(들):
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
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C18H20N4O2S · xC4H6O4
Molecular Weight:
356.44 (free base basis)
UNSPSC 코드:
12352202
NACRES:
NA.77
추천 제품
분석
≥98% (HPLC)
형태
powder
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
room temp
생화학적/생리학적 작용
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
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
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
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