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  3. Gomisin J

Gomisin J  (Synonyms: 戈米辛J)

目录号: HY-N0385 纯度: 99.97%
COA 产品使用指南 技术支持

Gomisin J 是一五味子来源的木脂素,可靶向 eNOSAMPK (LKB1CaMKIIβ)、fetuin-ANF-κBNrf2/HO-1 等多个靶点,且能通过血脑屏障。Gomisin J 通过激活 eNOS 增加 NO 生物利用度、激活 AMPK 通路调节脂代谢、抑制 fetuin-A 和 NF-κB 发挥抗炎作用、激活 Nrf2/HO-1 增强抗氧化能力等机制。Gomisin J 具有抗高血压、调节肝脂代谢、减轻脑缺血再灌注损伤等活性,可用于高血压、非酒精性脂肪肝、脑缺血再灌注损伤等研究。

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Gomisin J

Gomisin J Chemical Structure

CAS No. : 66280-25-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2478
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1 mg ¥990
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5 mg ¥2900
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10 mg ¥4640
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Gomisin J is a Schisandra chinensis-derived lignan that can inhibit multiple targets such as eNOS, AMPK (LKB1, CaMKIIβ), fetuin-A, NF-κB, Nrf2/HO-1, and can pass through the blood-brain barrier. Gomisin J increases NO bioavailability by activating eNOS, regulates lipid metabolism by activating the AMPK pathway, inhibits fetuin-A and NF-κB to exert anti-inflammatory effects, and activates Nrf2/HO-1 to enhance antioxidant capacity. Gomisin J has the activities of anti-hypertension, regulating liver lipid metabolism, and reducing cerebral ischemia-reperfusion injury, and can be used for research on hypertension, non-alcoholic fatty liver disease, cerebral ischemia-reperfusion injury, etc[1][2][3].

IC50 & Target[2]

AMPK

 

eNOS

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 100 μM
Compound: Gomisin J
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
[PMID: 18063366]
H9 IC50
23.2 μM
Compound: 3
Cytotoxicity against human H9 cells after 4 days
Cytotoxicity against human H9 cells after 4 days
[PMID: 17190445]
H9 EC50
3.9 μM
Compound: 3
Antiviral activity against HIV1 3B in H9 cells after 4 days by p24-antigen ELISA
Antiviral activity against HIV1 3B in H9 cells after 4 days by p24-antigen ELISA
[PMID: 17190445]
HCT-15 IC50
> 100 μM
Compound: Gomisin J
Antiproliferative activity against human HCT15 cells after 72 hrs by SRB assay
Antiproliferative activity against human HCT15 cells after 72 hrs by SRB assay
[PMID: 18063366]
HeLa IC50
> 100 μM
Compound: 4
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
[PMID: 23237974]
HL-60 IC50
> 160.9 μM
Compound: 10
Antioxidant activity in human HL60 cells assessed as inhibition of TPA-stimulated hydrogen peroxide induced DCFH-DA oxidation by fluorometric microplate assay
Antioxidant activity in human HL60 cells assessed as inhibition of TPA-stimulated hydrogen peroxide induced DCFH-DA oxidation by fluorometric microplate assay
[PMID: 16562834]
HL-60 IC50
54.8 μM
Compound: 10
Cytotoxicity against human HL60 cells by XTT assay
Cytotoxicity against human HL60 cells by XTT assay
[PMID: 16562834]
K562 IC50
> 100 μM
Compound: Gomisin J
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
[PMID: 18063366]
Lewis lung carcinoma cell line IC50
> 100 μM
Compound: 4
Cytotoxicity against mouse LLC cells after 72 hrs by MTT assay
Cytotoxicity against mouse LLC cells after 72 hrs by MTT assay
[PMID: 23237974]
MDA-MB-231 IC50
> 100 μM
Compound: Gomisin J
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
[PMID: 18063366]
SK-HEP1 IC50
> 100 μM
Compound: Gomisin J
Antiproliferative activity against human SK-HEP1 cells after 72 hrs by SRB assay
Antiproliferative activity against human SK-HEP1 cells after 72 hrs by SRB assay
[PMID: 18063366]
SMMC-7721 IC50
> 100 μM
Compound: 4
Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay
Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay
[PMID: 23237974]
SNU-638 IC50
> 100 μM
Compound: Gomisin J
Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay
Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay
[PMID: 18063366]
T47D IC50
> 100 μM
Compound: Gomisin J
Antiproliferative activity against human T47D cells after 72 hrs by SRB assay
Antiproliferative activity against human T47D cells after 72 hrs by SRB assay
[PMID: 18063366]
U-87MG ATCC IC50
> 100 μM
Compound: 4
Cytotoxicity against human U87 cells after 72 hrs by MTT assay
Cytotoxicity against human U87 cells after 72 hrs by MTT assay
[PMID: 23237974]
体外研究
(In Vitro)

Gomisin J (10-200 μM;24 h) 低剂量时 (≤50 μM),对 HepG2 细胞活力无显著影响[2]
Gomisin J (10-40 μM;24 h) 减少 HepG2 细胞中 Oleic acid (HY-N1446) 诱导的脂质积累和 TG 含量,并下调脂生成蛋白 (SREBP-1c、FAS),上调脂解蛋白 (PPARα、PGC-1α),激活 AMPK 及 ACC 磷酸化[2]
Gomisin J (10-40 μM;24 h) 在 HepG2 细胞中下调脂生成基因 (SREBP-1c、FAS等) 和炎症基因 (TNF-α、MCP-1等),上调脂解基因 (PPARα、CPT-1 等),且具有 LKB1 依赖性 AMPK 激活作用[2]

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

RT-PCR[2]

Cell Line: HepG2
Concentration: 10-40 μM
Incubation Time: 1 h pretreatment followed by 24 h Oleic acid (HY-N1446) treatment
Result: Decreased mRNA levels of SREBP-1c, FAS, ACC, HMGCR, DGAT1, TNF-α, MCP-1, NFKB1, and NFKB2.
Increased mRNA levels of PPARα, PPARδ, PGC-1α, ACOX1, CPT-1, and UCP2.
体内研究
(In Vivo)

Gomisin J (1 μg/kg/min 和 3 μg/kg/min;mini泵,皮下注射;持续给药;14 天) 在 C57BL/6 小鼠的 Ang II 诱导高血压模型中,减轻血压升高,恢复血浆 NO 代谢物水平和血管 NO 产生,减少血管 ROS 生成[1]
Gomisin J (5-80 mg/kg;腹腔注射;再灌注前单次给药;观察至再灌注后 48 h) 在 Wistar 大鼠的大脑中动脉闭塞/再灌注 (MCAO/R) 模型中,剂量依赖性降低神经功能评分、脑梗死体积和脑含水量,抑制海马神经元凋亡,减轻炎症和氧化应激[3]

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

Animal Model: Male Wistar rats (250-300 g) with middle cerebral artery occlusion/reperfusion (MCAO/R) model (occlusion for 2 h followed by reperfusion for 3, 6, 12, 24, or 48 h)[3]
Dosage: 5, 10, 20, 40, 80 mg/kg
Administration: Intraperitoneal injection, single administration before reperfusion, observed until 48 h after reperfusion
Result: Dose-dependently decreased neurological deficit scores, reduced cerebral infarct volume and brain water content, rescued the reduction in hippocampal neuron survival, inhibited apoptosis of ischemic tissues by regulating Bcl-XL, cleaved caspase-3 and Bax, alleviated inflammation by reducing p-p65, COX-2 and NO levels, and enhanced antioxidant capacity by promoting Nrf2 translocation, HO-1 expression, and activities of SOD, GSH-Px as well as GSH level.
分子量

388.45

Formula

C22H28O6

CAS 号
性状

固体

颜色

White to off-white

中文名称

戈米辛J

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 : 100 mg/mL (257.43 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 2.5743 mL 12.8717 mL 25.7433 mL
5 mM 0.5149 mL 2.5743 mL 5.1487 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)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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 (6.44 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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。
  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (6.44 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
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

g

每只动物的给药体积

μL

动物数量

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: 99.97%

参考文献

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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5743 mL 12.8717 mL 25.7433 mL 64.3583 mL
5 mM 0.5149 mL 2.5743 mL 5.1487 mL 12.8717 mL
10 mM 0.2574 mL 1.2872 mL 2.5743 mL 6.4358 mL
15 mM 0.1716 mL 0.8581 mL 1.7162 mL 4.2906 mL
20 mM 0.1287 mL 0.6436 mL 1.2872 mL 3.2179 mL
25 mM 0.1030 mL 0.5149 mL 1.0297 mL 2.5743 mL
30 mM 0.0858 mL 0.4291 mL 0.8581 mL 2.1453 mL
40 mM 0.0644 mL 0.3218 mL 0.6436 mL 1.6090 mL
50 mM 0.0515 mL 0.2574 mL 0.5149 mL 1.2872 mL
60 mM 0.0429 mL 0.2145 mL 0.4291 mL 1.0726 mL
80 mM 0.0322 mL 0.1609 mL 0.3218 mL 0.8045 mL
100 mM 0.0257 mL 0.1287 mL 0.2574 mL 0.6436 mL
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  • 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.

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