1. PI3K/Akt/mTOR MAPK/ERK Pathway
  2. mTOR Ribosomal S6 Kinase (RSK)
  3. Coronarin A

Coronarin A 是一种具有口服活性的天然物,可抑制 mTORC1S6K1 增加 IRS1 活性。Coronarin A 具有抗炎活性,也可用于糖尿病的研究。

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Coronarin A Chemical Structure

Coronarin A Chemical Structure

CAS No. : 119188-33-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Coronarin A is an orally active natural compound that inhibits mTORC1 and S6K1 to increase IRS1 activity. Coronarin A shows anti-inflammatory activity and can also be used for type 2 diabetes mellitus research[1].

IC50 & Target[1]

mTORC1

 

S6K1

 

体外研究
(In Vitro)

Coronarin A (3-30?μM; 4 or 12 h) stimulates glycogen synthesis through activating PI3K/Akt/GSK3β signaling and inhibits gluconeogenesis by activating ERK-dependent Wnt/β-catenin/TCF7L2 pathway in rat primary hepatocytes[1].
Coronarin A (1-30 μM; 4 h) increases tyrosine phosphorylation of IRS1 through inhibiting mTOR/S6K1 signaling[1].

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

Western Blot Analysis[1]

Cell Line: Primary rat hepatocytes
Concentration: 1, 3, 10 and 30 μM
Incubation Time: 4 h
Result: Increased the Akt and GSK3β phosphorylation dose-dependently. Dose-dependently stimulated the phosphorylation of both ERK1 and ERK2. Increased the phosphorylation of β-catenin and mitogen-activated protein kinase kinase (MEK). Dose-dependently enhanced the tyrosine phosphorylation of IRS1 at Tyr1222, whereas the serine phosphorylation of IRS1 was dose-dependently inhibited. Reduced the phosphorylation of mTOR, S6K1 and S6.

Cell Viability Assay[1]

Cell Line: Primary rat hepatocytes
Concentration: 1, 3, 10, 30, 100 and 300 μM
Incubation Time: 5.5 h or 12 h
Result: Showed no toxicity at 1-30 μM, decreased cell viability after 12 h incubation at 100 μM.
体内研究
(In Vivo)

Coronarin A (30 or 100 mg/kg; i.p. or p.o.; once daily for 22 days) ameliorates hyperglycemia in mice[1].
Coronarin A (100 mg/kg; p.o.; once daily for 22 days) inhibits the mTOR/S6K1 pathway to activate PI3K/Akt and ERK/β-catenin signaling in livers of ob/ob mice[1].
Pharmacokinetic properties of Coronarin A after single administrationa in ob/ob mice[1].

Coronarin A t1/2 (h) tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) AUC0-∞ (ng·h/mL) MRT (h)
i.p. 14.8 1.0 1073 4571 11045 21.7
p.o. 3.01 1.0 388 1694 1856 4.88

Data are presented as the mean of three mice.
aCoronarin A was intraperitoneally or orally administered at 30 mg/kg to ob/ob mice.

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

Animal Model: Male ob/ob mice[1]
Dosage: 30 mg/kg (IP) or 100 mg/kg (PO)
Administration: Oral or intraperitoneal administration, once daily for 22 days
Result: Significantly decreased the non-fasting and fasting blood glucose. Significantly reduced the serum insulin concentration at 15 min after glucose loading, reduced the average daily food intake while the body weight was unaffected. Increased hepatic glycogen content and the expression levels of gluconeogenic gene Pck1 and G6pc were significantly decreased.
Animal Model: Female ob/ob mice[1]
Dosage: 30 mg/kg
Administration: Intraperitoneal or oral administration (Pharmacokinetic Analysis)
Result: Intraperitoneal injection exhibited higher plasma exposure than oral gavage at the same dose of 30 mg/kg, with Cmax value of 1073 and 388 ng/mL, respectively.
分子量

300.44

Formula

C20H28O2

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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 10 mg/mL (33.28 mM; 超声加热助溶; 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 3.3285 mL 16.6423 mL 33.2845 mL
5 mM 0.6657 mL 3.3285 mL 6.6569 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。-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: ≥98.0%

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。-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 3.3285 mL 16.6423 mL 33.2845 mL 83.2113 mL
5 mM 0.6657 mL 3.3285 mL 6.6569 mL 16.6423 mL
10 mM 0.3328 mL 1.6642 mL 3.3285 mL 8.3211 mL
15 mM 0.2219 mL 1.1095 mL 2.2190 mL 5.5474 mL
20 mM 0.1664 mL 0.8321 mL 1.6642 mL 4.1606 mL
25 mM 0.1331 mL 0.6657 mL 1.3314 mL 3.3285 mL
30 mM 0.1109 mL 0.5547 mL 1.1095 mL 2.7737 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:
Coronarin A
目录号:
HY-N3628
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