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Humulone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Humulone图片
CAS NO:26472-41-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
律草酮
α-Lupulic acid
产品介绍
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。
生物活性

Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potentcyclooxygenase-2 (COX-2)inhibitor. Humulone acts as a positive modulator ofGABAAreceptorat low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic andapoptosis-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].

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].

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

性状

Oil

Formula

C21H30O5

CAS 号

26472-41-3

中文名称

律草酮

结构分类
  • Ketones, Aldehydes, Acids
来源
  • Plants
  • Moraceae
  • Humulus lupulusL.
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 : 50 mg/mL(137.95 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7589 mL13.7946 mL27.5893 mL
5 mM0.5518 mL2.7589 mL5.5179 mL
10 mM0.2759 mL1.3795 mL2.7589 mL
*

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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。