SB-334867freebase
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发布时间: 2024-07-15 12:36:50
CAS号:792173-99-0
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纯度: 99.0%
备货期: 10天
库存: 现货
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用途: SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.IC50 value: 7.2 (pKb) [1]Target: orexin OX1 receptor in vitro: SB-334867-A inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses (pK(B)=7.27+/-0.04 and 7.23+/-0.03 respectively, n=8), but had no effect on the UTP (3 microM)-induced calcium response in CHO-OX(1) cells. SB-334867-A (10 microM) also inhibited OX(2) mediated calcium responses (32.7+/-1.9% versus orexin-A) [1].in vivo: Single-unit recordings in anesthetized rats demonstrated the central effects of the selective orexin-1 receptor antagonist SB-334867 (2 mg/kg, intravenous), as it reversed the excitatory effects of orexin-A administration (6 microg, intracerebroventricular) on the activity of locus coeruleus (LC) cells [2]. The ICV injection of SB-334867 alone had no effect on the formalin-induced nociceptive behaviors. Pre-treatment with SB-334867 at a dose of 0.5 nmol significantly attenuated the analgesia induced by morphine (at dose 1.5mg/kg of morphine; interphase and phase 2B and at dose 3mg/kg of morphine just phase 2B of formalin test) [3]. Administered alone, SB-334867 (30 mg/kg, but not lower doses) significantly reduced food intake and most active behaviours (eating, grooming, sniffing, locomotion and rearing), while increasing resting. Pretreatment with SB-334867 dose-dependently blocked these effects of orexin-A, with significant antagonism evident at dose levels (3-10 mg/kg) below those required to produce intrinsic behavioural effects under present test conditions in rats [4].Toxicity: Acute systemic treatment with the selective orexin-1 (OX1R) antagonist SB-334867 reduces food intake in rats, an effect associated with an acceleration in behavioural satiety and unrelated to gross behavioural disruption, alterations in palatability, or toxicity. 物理化学性质: CAS号:792173-99-0 常用中文名:1-(2-甲基苯并[D]噁唑-6-基)-3-(1,5-萘啶-4-基)脲 常用英文名:SB 334867 分子式:C17H13N5O2 分子量:319.317 密度:1.4±0.1 g/cm3 沸点:549.5±58.0 °C at 760 mmHg 熔点:N/A 闪点:286.1±32.3 °C 储存条件:-20℃
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公司名:上海化源世纪贸易有限公司 推荐
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公司名:上海源溪生物科技有限公司
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公司名:上海脉铂医药科技有限公司
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公司名:上海阿拉丁生化科技股份有限公司
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¥639.9/5mg
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公司名:上海创赛科技有限公司
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¥651.0/5mg
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2022-11-29 价格:¥需询单
2020-12-08 价格:¥1100.0
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