1. Anti-infection PI3K/Akt/mTOR NF-κB
  2. Parasite PI3K Akt mTOR NF-κB
  3. Lupenone

Lupenone 是一种具有口服活性的可从 Musa basjoo 中分离出的 lupine 型三萜类化合物。Lupenone Lupenone 可通过 PI3K/Akt/mTORNF-κB 信号通路发挥作用。Lupenone 具有抗炎、抗病毒、抗糖尿病和抗癌活性。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Lupenone Chemical Structure

Lupenone Chemical Structure

CAS No. : 1617-70-5

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Lupenone is an orally active lupine-type triterpenoid that can be isolated from Musa basjoo. Lupenone Lupenone plays a role through the PI3K/Akt/mTOR and NF-κB signaling pathways. Lupenone has anti-inflammatory, antiviral, antidiabetic and anticancer activities[1][2][3].

IC50 & Target

Trypanosoma

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
B16 ED50
0.35 μM
Compound: 2
Induction of melanogenesis in mouse B16 2F2 cells assessed as intracellular melanin content after 3 days
Induction of melanogenesis in mouse B16 2F2 cells assessed as intracellular melanin content after 3 days
[PMID: 12027734]
B16 IC50
25.4 μM
Compound: 2
Growth inhibition of mouse B16 2F2 cells after 3 days
Growth inhibition of mouse B16 2F2 cells after 3 days
[PMID: 12027734]
CHO EC50
> 10 μM
Compound: Lupenone
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
[PMID: 19911773]
COS-1 EC50
0 μM
Compound: Lupenone
Agonist activity at human FXR expressed in COS1 cells by luciferase reporter gene assay
Agonist activity at human FXR expressed in COS1 cells by luciferase reporter gene assay
[PMID: 19911773]
DU-145 CC50
> 500 μM
Compound: 4
Cytotoxic activity in human DU145 cells by sulforhodamine B assay
Cytotoxic activity in human DU145 cells by sulforhodamine B assay
[PMID: 29120172]
DU-145 IC50
> 500 μM
Compound: 4
Antiproliferative activity in human DU145 cells by sulforhodamine B assay
Antiproliferative activity in human DU145 cells by sulforhodamine B assay
[PMID: 29120172]
HEK293 CC50
> 500 μM
Compound: 4
Cytotoxic activity in HEK293 cells by sulforhodamine B assay
Cytotoxic activity in HEK293 cells by sulforhodamine B assay
[PMID: 29120172]
HEK293 IC50
> 500 μM
Compound: 4
Antiproliferative activity in HEK293 cells by sulforhodamine B assay
Antiproliferative activity in HEK293 cells by sulforhodamine B assay
[PMID: 29120172]
HeLa IC50
> 10 μg/mL
Compound: lupenone
Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
[PMID: 16038541]
HeLa CC50
> 500 μM
Compound: 4
Cytotoxic activity in human HeLa cells by sulforhodamine B assay
Cytotoxic activity in human HeLa cells by sulforhodamine B assay
[PMID: 29120172]
HeLa IC50
> 500 μM
Compound: 4
Antiproliferative activity in human HeLa cells by sulforhodamine B assay
Antiproliferative activity in human HeLa cells by sulforhodamine B assay
[PMID: 29120172]
HEp-2 IC50
> 10 μg/mL
Compound: lupenone
Cytotoxicity against human Hep2 cells after 48 hrs by MTT assay
Cytotoxicity against human Hep2 cells after 48 hrs by MTT assay
[PMID: 16038541]
HEp-2 CC50
> 500 μM
Compound: 4
Cytotoxic activity in human Hep2 cells by sulforhodamine B assay
Cytotoxic activity in human Hep2 cells by sulforhodamine B assay
[PMID: 29120172]
HEp-2 IC50
> 500 μM
Compound: 4
Antiproliferative activity in human Hep2 cells by sulforhodamine B assay
Antiproliferative activity in human Hep2 cells by sulforhodamine B assay
[PMID: 29120172]
J774.A1 IC50
38.8 μM
Compound: 2
Antiinflammatory activity in mouse J774A1 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess method
Antiinflammatory activity in mouse J774A1 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess method
[PMID: 24909081]
KB CC50
> 500 μM
Compound: 4
Cytotoxic activity in human KB cells by sulforhodamine B assay
Cytotoxic activity in human KB cells by sulforhodamine B assay
[PMID: 29120172]
KB IC50
> 500 μM
Compound: 4
Antiproliferative activity in human KB cells by sulforhodamine B assay
Antiproliferative activity in human KB cells by sulforhodamine B assay
[PMID: 29120172]
L6 IC50
> 90 μM
Compound: 10
Cytotoxicity against rat L6 cells after 72 hrs by microplate fluorimetry
Cytotoxicity against rat L6 cells after 72 hrs by microplate fluorimetry
[PMID: 21438586]
MCF7 CC50
> 500 μM
Compound: 4
Cytotoxic activity in human MCF7 cells by sulforhodamine B assay
Cytotoxic activity in human MCF7 cells by sulforhodamine B assay
[PMID: 29120172]
MCF7 IC50
> 500 μM
Compound: 4
Antiproliferative activity in human MCF7 cells by sulforhodamine B assay
Antiproliferative activity in human MCF7 cells by sulforhodamine B assay
[PMID: 29120172]
MDA-MB-231 CC50
> 500 μM
Compound: 4
Cytotoxic activity in human MDA-MB-231 cells by sulforhodamine B assay
Cytotoxic activity in human MDA-MB-231 cells by sulforhodamine B assay
[PMID: 29120172]
MDA-MB-231 IC50
> 500 μM
Compound: 4
Antiproliferative activity in human MDA-MB-231 cells by sulforhodamine B assay
Antiproliferative activity in human MDA-MB-231 cells by sulforhodamine B assay
[PMID: 29120172]
RAW264.7 IC50
> 0.4 μM
Compound: lupenone
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide release after 24 hrs
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide release after 24 hrs
[PMID: 20192236]
RAW264.7 IC50
38.5 μM
Compound: 2
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess method
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess method
[PMID: 24909081]
SiHa CC50
> 500 μM
Compound: 4
Cytotoxic activity in human SiHa cells by sulforhodamine B assay
Cytotoxic activity in human SiHa cells by sulforhodamine B assay
[PMID: 29120172]
SiHa IC50
> 500 μM
Compound: 4
Antiproliferative activity in human SiHa cells by sulforhodamine B assay
Antiproliferative activity in human SiHa cells by sulforhodamine B assay
[PMID: 29120172]
Vero IC50
> 10 μg/mL
Compound: lupenone
Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay
[PMID: 16038541]
Vero CC50
> 500 μM
Compound: 4
Cytotoxic activity in African green monkey Vero cells by sulforhodamine B assay
Cytotoxic activity in African green monkey Vero cells by sulforhodamine B assay
[PMID: 29120172]
Vero IC50
> 500 μM
Compound: 4
Antiproliferative activity in African green monkey Vero cells by sulforhodamine B assay
Antiproliferative activity in African green monkey Vero cells by sulforhodamine B assay
[PMID: 29120172]
体外研究
(In Vitro)

Lupenone (40 μM, 1 h) 通过 PI3K/Akt/mTOR 信号通路保护神经母细胞瘤 SH-SY5y 细胞免受甲基苯丙胺诱导的凋亡细胞死亡[1]

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

Cell Viability Assay[1]

Cell Line: SH-SY5y
Concentration: 5, 10. 20, 40 μM
Incubation Time: 24 h
Result: Did not cause significant cell death at different concentrations.

Apoptosis Analysis[1]

Cell Line: SH-SY5y
Concentration: 40 μM
Incubation Time: 1 h
Result: Reduced the population of annexinV/PI-positive cells (early apoptotic cells) and annexinV positive cells (total apoptotic cells).

Western Blot Analysis[1]

Cell Line: SH-SY5y
Concentration: 40 μM
Incubation Time: 1 h
Result: Increased the expression of anti-apoptotic proteins, including bcl-2 and caspases such as caspase 3, caspase 7, and caspase 8.
Recuperate the phosphorylation level of PI3K and Akt.
Inhibited the translocation of p65 from the cytosol to the nucleus, IκBα degradation, and IκBα phosphorylation.
体内研究
(In Vivo)

Lupenone (6, 12, 24 mg/kg/day, 灌胃, 连续 6 周) 通过调节 NF-κB 通路介导的炎症和 TGF-β1/Smad/ CTGF 相关纤维化改善 2 型糖尿病肾病[2]

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

Animal Model: Spontaneous type 2 diabetic nephropathy db/db mouse models[1]
Dosage: 6, 12, 24 mg/kg
Administration: i.g.
Result: Maintained the fasting blood glucose.
Reduced glycosylated hemoglobin, insulin, and 24 h proteinuria levels.
Regulated changes in biochemical indicators
分子量

424.70

Formula

C30H48O

CAS 号
性状

固体

颜色

White to off-white

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: 

Ethanol 中的溶解度 : 10 mg/mL (23.55 mM; 超声助溶 (<60°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3546 mL 11.7730 mL 23.5460 mL
5 mM 0.4709 mL 2.3546 mL 4.7092 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% EtOH    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1 mg/mL (2.35 mM); 澄清溶液

    此方案可获得 ≥ 1 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 EtOH 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% EtOH    90% Corn Oil

    Solubility: ≥ 1 mg/mL (2.35 mM); 澄清溶液

    此方案可获得 ≥ 1 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 玉米油中,混合均匀。

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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.74%

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
Ethanol 1 mM 2.3546 mL 11.7730 mL 23.5460 mL 58.8651 mL
5 mM 0.4709 mL 2.3546 mL 4.7092 mL 11.7730 mL
10 mM 0.2355 mL 1.1773 mL 2.3546 mL 5.8865 mL
15 mM 0.1570 mL 0.7849 mL 1.5697 mL 3.9243 mL
20 mM 0.1177 mL 0.5887 mL 1.1773 mL 2.9433 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.

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产品名称:
Lupenone
目录号:
HY-N2590
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