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3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺

更新时间:2024-07-15 12:32:53 采购访问:15次

常用名 3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺 CAS号 174635-69-9
价格 纯度 99.0%
备货期 10天 库存 现货
 产品详情(用途,包装等)
用途:
SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier.IC50 Value: 4.4 nM ( Ki for hNK-3 receptor); 250 nM( Ki for hNK-2 receptor) [1]Target: NK3 Receptorin vitro: SB-222200 inhibited (125)I-[MePhe(7)]neurokinin B (NKB) binding to Chinese hamster ovary (CHO) cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K(i) = 4.4 nM and antagonized NKB-induced Ca(2+) mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC(50) = 18.4 nM. SB-222200 was selective for hNK-3 receptors compared with hNK-1 (K(i) > 100,000 nM) and hNK-2 receptors (K(i) = 250 nM). n HEK 293 cells transiently expressing murine NK-3 receptors (HEK 293-mNK-3R), SB-222200 inhibited binding of (125)I-[MePhe(7)]NKB (K(i) = 174 nM) and antagonized NKB (1 nM)-induced calcium mobilization (IC(50) = 265 nM) [1].in vivo: In mice oral administration of SB-222200 produced dose-dependent inhibition of behavioral responses induced by i.p. or intracerebral ventricular administration of the NK-3 receptor-selective agonist, senktide, with ED(50) values of approximately 5 mg/kg. SB-222200effectively crossed the blood-brain barrier in the mouse and rat. The inhibitory effect of SB-222200 against senktide-induced behavioral responses in the mouse correlated significantly with brain, but not plasma, concentrations of the compound. Pharmacokinetic evaluation of SB-222200 in rat after oral administration (8 mg/kg) indicated sustained plasma concentrations (C(max) = about 400 ng/ml) and bioavailability of 46% [1].
物理化学性质:
CAS号:174635-69-9
常用中文名:3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺
常用英文名:SB-222200
分子式:C26H24N2O
分子量:380.48200
密度:1.142g/cm3
沸点:553.5ºC at 760 mmHg
熔点:N/A
闪点:288.6ºC
储存条件:2-8℃

供应商信息

上海念兴实业有限公司 认证供应商

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联系人电话:0086-021-52280163
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参考价格:$172/10mM*1mLinDMSO
其他供应商价格:
2022-03-04 SB-222200
价格:¥898.9
2021-02-06 SB-222200
价格:¥5599.0

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