Stachydrine(Synonyms: 水苏碱)

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Stachydrine (Synonyms: 水苏碱) 纯度: ≥98.0%

Stachydrine 是中国草本植物益母草的主要成分,用于促进血液循环和消除血瘀。Stachydrine 可抑制 NF-κB 信号通路。

Stachydrine(Synonyms: 水苏碱)

Stachydrine Chemical Structure

CAS No. : 471-87-4

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生物活性

Stachydrine is a major constituent of Chinese herb leonurus heterophyllus sweet used to promote blood circulation and dispel blood stasis. Stachydrine can inhibit the NF-κB signal pathway.

IC50 & Target

p65

 

Human Endogenous Metabolite

 

体外研究
(In Vitro)

Stachydrine can inhibit the NF-κB signal pathway, and this may be related to the mechanism of anti-hypertrophic. Intervention of stachydrine significantly suppresses the level of p-IκB protein in the cytosol and NF-κB protein in the nucleus [1]. Tissue factor mRNA is decreased in stachydrine-treated human umbilical vein endothelial cells. Stachydrine attenuates the decline of human umbilical vein endothelial cells viability and the increase of LDH activity induced by anoxia-reoxygenation[2]. A dose dependent decrease in expression of mRNA, and protein levels are observed in stachydrine-treated human prostate cancer cells (PC-3 and LNcaP)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Stachydrine attenuates norepinephrine-induced cardiomyocyte hypertrophy and has potential protective effects against β-adrenergic receptor induced Ca2+ mishandling[4]. Stachydrine treatment reduces the expressions of PERK, CHOP, and caspase-3 in the endoplasmic reticulum stress-related apoptosis pathway[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

143.18

Formula

C7H13NO2

CAS 号

471-87-4

中文名称

水苏碱

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 100 mg/mL (698.42 mM; Need ultrasonic)

DMSO : 100 mg/mL (698.42 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 6.9842 mL 34.9211 mL 69.8422 mL
5 mM 1.3968 mL 6.9842 mL 13.9684 mL
10 mM 0.6984 mL 3.4921 mL 6.9842 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°C, 6 months; -20°C, 1 month。-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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 110 mg/mL (768.26 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (17.46 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (17.46 mM,饱和度未知) 的澄清溶液。

    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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (17.46 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (17.46 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (17.46 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (17.46 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Guo W, et al. Effect of Leonurus stachydrine on myocardial cell hypertrophy. Zhong Yao Cai. 2012 Jun;35(6):940-3.

    [2]. Yin J, et al. Stachydrine, a major constituent of the Chinese herb leonurus heterophyllus sweet, ameliorates human umbilical vein endothelial cells injury induced by anoxia-reoxygenation. Am J Chin Med. 2010;38(1):157-71.

    [3]. Rathee P, et al. In vitro anticancer activity of stachydrine isolated from Capparis decidua on prostate cancer cell lines. Nat Prod Res. 2012;26(18):1737-40.

    [4]. Zhang C, et al. Effects of stachydrine on norepinephrine-induced neonatal rat cardiac myocytes hypertrophy and intracellular calcium transients. BMC Complement Altern Med. 2014 Dec 8;14:474.

    [5]. Zhang C, et al. Effect of stachydrine on endoplasmic reticulum stress-induced apoptosis in rat kidney after unilateral ureteral obstruction. J Asian Nat Prod Res. 2013;15(4):373-81.

Cell Assay
[3]

Cytotoxicity is determined by colorimetric MTT cleavage assay. Briefly, human umbilical vein endothelial cells (HUVECs) are plated in triplicate in 96-well culture plates, and treated with different final concentrations (0.01, 0.1, 1, 10, 100 μM) of stachydrine respectively for 24 hours. After incubation, culture media are discarded and new culture media containing 0.5mg/mL of MTT are added. The plates are further incubated at 37°C for 4 hours. After the incubation, culture media are discarded and 0.1 mL of dimethyl sulfoxide (DMSO) is added to each well to solubilize the formazine crystals. The absorbance (OD) is measured at 540 nm using a microplate reader[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[5]

Rats: Ventricular myocytes from 1-day-old Wistar rats are isolated and cultured in DMEM/F12 with 1 μM norepinephrine in the presence or absence of 10 μM stachydrine for 72 h. Cardiomyocytes hypertrophy is evaluated by cell surface area, total protein/DNA content, β/α-MHC mRNA ratio. While calcium handling function is evaluated by Ca2+-transient amplitude and decay, SERCA2a activity and expression, PLN expression and phosphorylation. β1-adrenergic receptor system activation is evaluated by the content of cAMP and the activation of PKA[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Guo W, et al. Effect of Leonurus stachydrine on myocardial cell hypertrophy. Zhong Yao Cai. 2012 Jun;35(6):940-3.

    [2]. Yin J, et al. Stachydrine, a major constituent of the Chinese herb leonurus heterophyllus sweet, ameliorates human umbilical vein endothelial cells injury induced by anoxia-reoxygenation. Am J Chin Med. 2010;38(1):157-71.

    [3]. Rathee P, et al. In vitro anticancer activity of stachydrine isolated from Capparis decidua on prostate cancer cell lines. Nat Prod Res. 2012;26(18):1737-40.

    [4]. Zhang C, et al. Effects of stachydrine on norepinephrine-induced neonatal rat cardiac myocytes hypertrophy and intracellular calcium transients. BMC Complement Altern Med. 2014 Dec 8;14:474.

    [5]. Zhang C, et al. Effect of stachydrine on endoplasmic reticulum stress-induced apoptosis in rat kidney after unilateral ureteral obstruction. J Asian Nat Prod Res. 2013;15(4):373-81.

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