Yangonin
(Synonyms: 甲氧醉椒素) 目录号 : GC31809
A kavalactone with affinity for the CB1 receptor
Cas No.:500-62-9
Sample solution is provided at 25 µL, 10mM.
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Yangonin is a natural kavalactone from the kava plant, P. methysticum. It enhances the binding of bicuculline at the γ-amino butyric acid (GABA) receptor GABAA at 1.0 ?M.1 Yangonin also binds the central cannabinoid (CB1) receptor with a Ki value of 0.72 ?M, but whether it serves as an agonist or antagonist at this receptor remains to be determined.2 Yangonin blocks the activation of NF-κB by TNF-α.3 It also inhibits anchorage-dependent and independent growth of bladder cancer cell lines through induction of autophagic cell death (IC50s = 15-59 mg/mL).4
1.Boonen, G., and H?berlein, H.Influence of genuine kavapyrone enantiomers on the GABAA binding sitePlanta Med.64(6)504-506(1998) 2.Ligresti, A., Villano, R., Allará, M., et al.Kavalactones and the endocannabinoid system: The plant-derived yangonin is a novel CB1 receptor ligandPharmacol. Res.66(2)163-169(2012) 3.Ma, J., Liang, H., Jin, H.R., et al.Yangonin blocks tumor necrosis factor-α-induced nuclear factor-κB-dependent transcription by inhibiting the transactivation potential of the RelA/p65 subunitJ. Pharmacol. Sci.118(4)447-454(2012) 4.Zhongbo, L., U-Syn, H., Ke, Y., et al.Kavalactone yangonin induces autophagy and sensitizes bladder cancer cells to flavokawain A and docetaxel via inhibition of the mTOR pathwayJ. Biomed. Res.(2017)
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Cell experiment: |
HeLa cells are seeded at 1×105 cells/mL in 96-well plates containing 100 μL of DMEM medium with 10% FBS and incubated overnight. Yangonin is dissolved in DMSO and DMSO is added to all plates to compensate the same volume of DMSO. After 24 h, the cells are pretreated with different concentrations of Yangonin (0.1-3 μM) for 1 h, followed by stimulation with or without TNF-α for 24 h. Subsequently, cells are cultured with MTT solution (5 mg/mL) for 3 h. The viable cells convert MTT to formazan, which generates a blue-purple color after dissolving in 150 μL of DMSO. The absorbance at 570 nm is measured by an ELISA plate reader[2]. |
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References: [1]. Ligresti A, et al. Kavalactones and the endocannabinoid system: the plant-derived yangonin is a novel CB1 receptor ligand. Pharmacol Res. 2012 Aug;66(2):163-9. |
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| Cas No. | 500-62-9 | SDF | |
| 别名 | 甲氧醉椒素 | ||
| Canonical SMILES | O=C1C=C(OC)C=C(/C=C/C2=CC=C(OC)C=C2)O1 | ||
| 分子式 | C15H14O4 | 分子量 | 258.27 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 5 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8719 mL | 19.3596 mL | 38.7192 mL |
| 5 mM | 0.7744 mL | 3.8719 mL | 7.7438 mL |
| 10 mM | 0.3872 mL | 1.936 mL | 3.8719 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet