Humulone (Synonyms: 律草酮; α-Lupulic acid)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物,专注于信号通路和疾病研究领域。
Humulone  (Synonyms: 律草酮; α-Lupulic acid) 纯度: 99.33%

Humulone (α-Lupulic acid) 是一种异戊二烯化间苯三酚衍生物,是一种有效的环氧合酶 2 (COX-2) 抑制剂。Humulone 在低微摩尔浓度下作为 GABAA 受体的正调节剂。Humulone 是一种骨吸收抑制剂。Humulone 具有抗氧化、抗血管生成和诱导细胞凋亡的特性。

Humulone                                          (Synonyms: 律草酮; α-Lupulic acid)

Humulone Chemical Structure

CAS No. : 26472-41-3

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生物活性

Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties[1][2][3].

IC50 & Target[1][2][3]

COX-2

 

体外研究
(In Vitro)

Humulone (0.1, 1, 10, 100, 1000, 10000 nM; for 12 h) with with 10 ng/ml TNFα dose-dependently decreases the amount of released PGE2 with an IC50 of about 30 nM in MC3T3-E1 cells. Humulone reduces cyclooxygenase activity of the TNFK-treated cells[1].
Humulone (0.1-10000 nM; for 12 h) suppresses the TNFα-induced increase of cyclooxygenase-2 mRNA[1].
Humulone hardly affects the cyclooxygenase-1 activity below 10 μM, whereas inhibits the cyclooxygenase-2 activity with an IC50 of about 1.6 μM in MC3T3-E1 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Humulone 相关抗体:

体内研究
(In Vivo)

Humulone (10 or 20 mg/kg; IP; single dose) shortens sleep onset and increases the duration of sleep induced by pentobarbital and decreases the spontaneous locomotion in open field at 20 mg/kg[2].
Humulone (10 μmol; applied topically to the dorsal shaved area) pre-treatment significantly inhibited TPA (10 nmol)-induced COX-2 expression in Female ICR mice (6-7 weeks of age) skin[3].
Humulone (1, 10 μmol; applied topical; pre-treatment 30 min) suppresses TPA-induced NF-κB DNA binding. Humulone attenuates TPA-stimulated nuclear translocation of p65 and p50 subunit proteins of NF-κB[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/cAnNRj mice (9-11 weeks of age)[2]
Dosage: 10 or 20 mg/kg
Administration: IP; pre-treatment before sodium pentobarbital (35 mg/kg; i.p.) and ethanol (3.5 g/kg)
Result: Significantly decreased the latency and prolonged the duration of sleep induced by pentobarbital at 20 mg/kg dose. These effects were not observed at a lower dose of 10 mg/kg.
Showed no effect on the onset of sleep induced by ethanol, but significantly increased sleep duration dose-dependently.

分子量

362.46

Formula

C21H30O5

CAS 号

26472-41-3

性状

油状物

颜色

Light yellow to yellow

中文名称

律草酮

结构分类
  • Ketones, Aldehydes, Acids
初始来源
  • 植物
  • 桑科
  • 啤酒花
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 50 mg/mL (137.95 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7589 mL 13.7946 mL 27.5893 mL
5 mM 0.5518 mL 2.7589 mL 5.5179 mL
10 mM 0.2759 mL 1.3795 mL 2.7589 mL

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* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

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给药剂量

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纯度 & 产品资料

纯度: 99.33%

Data Sheet (607 KB) SDS (252 KB)

COA (264 KB) HNMR (266 KB) LCMS (264 KB)

产品使用指南 (1538 KB)

参考文献
  • [1]. K Yamamoto, et al. Suppression of cyclooxygenase-2 gene transcription by humulon of beer hop extract studied with reference to glucocorticoid. FEBS Lett. 2000 Jan 14;465(2-3):103-6.  [Content Brief]

    [2]. Ali Y Benkherouf, et al. Humulone Modulation of GABA A Receptors and Its Role in Hops Sleep-Promoting Activity. Front Neurosci. 2020 Oct 14;14:594708.  [Content Brief]

    [3]. Jung-Chul Lee, et al. Humulone inhibits phorbol ester-induced COX-2 expression in mouse skin by blocking activation of NF-kappaB and AP-1: IkappaB kinase and c-Jun-N-terminal kinase as respective potential upstream targets. Carcinogenesis. 2007 Jul;28(7):  [Content Brief]

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