Yangonin (Synonyms: 甲氧醉椒素)

目录号: HY-N0919 纯度: 99.79%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Yangonin 对人重组大麻素 CB1 受体具有高的亲和力，IC₅₀ 和 K_i 分别为 1.79 μM 和 0.72 μM。

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Yangonin Chemical Structure

CAS No. : 500-62-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1818	In-stock
1 mg	￥640	In-stock
5 mg	￥1400	In-stock
10 mg	￥2300	In-stock
50 mg		询价
100 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Yangonin:

Yangonin (Standard) 询价

MCE 顾客使用本产品发表的 1 篇科研文献

•Inflammopharmacology. 2022 Apr 22. [Abstract]

Yangonin 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Cannabinoid Receptor 亚型特异性产品:

查看所有亚型

CB1 CB2

查看 NF-κB 亚型特异性产品:

查看所有亚型

NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC₅₀ and a K_i of 1.79 μM and 0.72 μM, respectively.

IC₅₀ & Target^[1]^[2]

CB1

1.79 μM (IC₅₀)

CB1

0.72 μM (Ki)

RelA

体外研究
(In Vitro)

Yangonin is one of the six major kavalactones found in Piper methysticum.Yangonin potently inhibits NF-κB activation through suppression of the transcriptional activity of the RelA/p65 subunit of NF-κB. Yangonin significantly inhibits the induced expression of the NF-κB-reporter gene. However, Yangonin does not interfere with TNF-α-induced inhibitor of κBα (IκBα) degradation, p65 nuclear translocation, and DNA-binding activity of NF-κB. Yangonin inhibits not only the induced NF-κB activation by overexpression of RelA/p65, but also transactivation activity of RelA/p65. Yangonin does not inhibit TNF-α-induced activation of p38, but it significantly impairs activation of ERK 1/2 and stress-activated protein kinase/JNK^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

258.27

Formula

C₁₅H₁₄O₄

CAS 号

500-62-9

性状

固体

颜色

Light yellow to yellow

中文名称

甲氧醉椒素

结构分类

初始来源

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (96.80 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	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	1.9360 mL	3.8719 mL

查看完整储备液配制表

* 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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (9.68 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

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

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.79%

选择批次：

Data Sheet (624 KB) SDS (252 KB)

COA (283 KB) HNMR (266 KB) LCMS (265 KB)

产品使用指南 (1538 KB)

参考文献

[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. [Content Brief]

[2]. Ma J, et al. Yangonin blocks tumor necrosis factor-α-induced nuclear factor-κB-dependent transcription by inhibiting the transactivation potential of the RelA/p65 subunit. J Pharmacol Sci. 2012;118(4):447-54. [Content Brief]

[3]. Wruck CJ, et al. Kavalactones protect neural cells against amyloid beta peptide-induced neurotoxicity via extracellular signal-regulated kinase 1/2-dependent nuclear factor erythroid 2-related factor 2 activation. Mol Pharmacol. 2008 Jun;73(6):1785-95. [Content Brief]

Cell Assay ^[2]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[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. [Content Brief] [2]. Ma J, et al. Yangonin blocks tumor necrosis factor-α-induced nuclear factor-κB-dependent transcription by inhibiting the transactivation potential of the RelA/p65 subunit. J Pharmacol Sci. 2012;118(4):447-54. [Content Brief] [3]. Wruck CJ, et al. Kavalactones protect neural cells against amyloid beta peptide-induced neurotoxicity via extracellular signal-regulated kinase 1/2-dependent nuclear factor erythroid 2-related factor 2 activation. Mol Pharmacol. 2008 Jun;73(6):1785-95. [Content Brief]

Cell Assay
^[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[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. [Content Brief]

[2]. Ma J, et al. Yangonin blocks tumor necrosis factor-α-induced nuclear factor-κB-dependent transcription by inhibiting the transactivation potential of the RelA/p65 subunit. J Pharmacol Sci. 2012;118(4):447-54. [Content Brief]

[3]. Wruck CJ, et al. Kavalactones protect neural cells against amyloid beta peptide-induced neurotoxicity via extracellular signal-regulated kinase 1/2-dependent nuclear factor erythroid 2-related factor 2 activation. Mol Pharmacol. 2008 Jun;73(6):1785-95. [Content Brief]

Yangonin 相关分类

Inflammation/Immunology

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.8719 mL	19.3596 mL	38.7192 mL	96.7979 mL
	5 mM	0.7744 mL	3.8719 mL	7.7438 mL	19.3596 mL
	10 mM	0.3872 mL	1.9360 mL	3.8719 mL	9.6798 mL
	15 mM	0.2581 mL	1.2906 mL	2.5813 mL	6.4532 mL
	20 mM	0.1936 mL	0.9680 mL	1.9360 mL	4.8399 mL
	25 mM	0.1549 mL	0.7744 mL	1.5488 mL	3.8719 mL
	30 mM	0.1291 mL	0.6453 mL	1.2906 mL	3.2266 mL
	40 mM	0.0968 mL	0.4840 mL	0.9680 mL	2.4199 mL
	50 mM	0.0774 mL	0.3872 mL	0.7744 mL	1.9360 mL
	60 mM	0.0645 mL	0.3227 mL	0.6453 mL	1.6133 mL
	80 mM	0.0484 mL	0.2420 mL	0.4840 mL	1.2100 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Yangonin500-62-9甲氧醉椒素Cannabinoid ReceptorNF-κBAutophagyNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Yangonin (Synonyms: 甲氧醉椒素)

Customer Review

Other Forms of Yangonin:

MCE 顾客使用本产品发表的 1 篇科研文献