SB-334867 hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SB-334867是orexin-1受体的一个选择性拮抗剂[1]。
Orexin-A和orexin-B是从大鼠下丘脑分离的两个肽。它们参与一些生理功能(如喂养控制、能量代谢和醒睡周期)的调节。SB-334867可以抑制CHO-OX1细胞中orexin-A和orexin-B诱导的钙反应,pKB值分别为7.27和7.23。SB-334867对OX1受体的选择性大于OX2受体。它对CHO-OX2细胞中orexin-A和orexin-B诱导的钙反应的抑制分别为32.7%和22%。此外,发现SB-334867可降低orexin-A以及禁食诱导的食物吸收。它的急性厌食效应与所有活跃行为的显著降低有关[1,2]。
参考文献:
[1]. Smart D, Sabido-David C, Brough S J, et al. SB-334867-A: the first selective orexin-1 receptor antagonist. British journal of pharmacology, 2001, 132(6): 1179-1182.
[2]. Rodgers R J, Halford J C G, Nunes de Souza R L, et al. SB-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-A in rats. European Journal of Neuroscience, 2001, 13(7): 1444-1452.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 355.78 |
Cas No. | 249889-64-3 |
Formula | C17H14ClN5O2 |
Solubility | insoluble in H2O; ≥2.72 mg/mL in EtOH with ultrasonic; ≥5.2 mg/mL in DMSO with gentle warming |
Chemical Name | 1-(2-methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea hydrochloride |
SDF | Download SDF |
Canonical SMILES | O=C(NC1=CC=NC2=CC=CN=C12)NC3=CC=C4N=C(C)OC4=C3.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
CHO-OX1和CHO-OX2细胞 |
溶解方法 |
在DMSO中的溶解度>5.2mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
100 pM-10 μM |
应用 |
在CHO-OX1细胞中,SB-334867-A(100pM-10μM)以浓度依赖性方式抑制食欲肽A(10nM)和食欲素-B(100nM)诱导的钙反应,pKB值分别为7.27±0.04和7.23±0.03。 在CHO-OX2细胞中,SB-334867-A也将食欲肽A(10nM)和食欲肽B(10nM)诱导的钙反应分别抑制32.7±1.9和22.0±4.0%。 |
动物实验[2]: | |
动物模型 |
成年雄性Lister hooded大鼠 |
剂量 |
3.0, 10.0和30.0 mg/kg, 腹腔注射 |
应用 |
在成年雄性Lister hooded大鼠,SB-334867显著减少食物摄入和最活跃的行为(饮食,梳理,嗅闻,运动和哺育),同时增加休息。SB-334867剂量依赖性地阻断了食欲素A的作用,如刺激食物摄入,增加梳理和延缓行为饱腹感发作。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Smart D, Sabido-David C, Brough S J, et al. SB-334867-A: the first selective orexin-1 receptor antagonist. British journal of pharmacology, 2001, 132(6): 1179-1182. [2] Rodgers R J, Halford J C G, Nunes de Souza R L, et al. SB-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-A in rats. European Journal of Neuroscience, 2001, 13(7): 1444-1452. |
质量控制和MSDS
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