Coronarin A
Based on 1 Customer Validation
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : ≥98.0%
- CAS 番号: 119188-33-9
- 分子式: C20H28O2
- 分子量:300.44
-
保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
製品説明
IC50 & Target
[1]|
mTORC1 |
S6K1 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
4.22 μg/mL
Compound: 1
|
Growth inhibitory activity against human umbilical vein endothelial cells (HUVEC) proliferation using MTT colorimetric method
Growth inhibitory activity against human umbilical vein endothelial cells (HUVEC) proliferation using MTT colorimetric method
|
[PMID: 12781184] |
| V79 | IC50 |
1.65 μg/mL
Compound: coronarin A
|
Cytotoxicity against Chinese hamster V79 cells
Cytotoxicity against Chinese hamster V79 cells
|
[PMID: 9834161] |
体外実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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 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.
体内実験
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.
MedChemExpress (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.
化学情報
-
CAS 番号 119188-33-9
-
性状 Solid
-
分子量 300.44
-
分子式 C20H28O2
-
Color White to off-white
-
SMILES
C[C@@]1([C@H]2/C=C/C3=COC=C3)[C@@](C(C)(CCC1)C)([H])C[C@H](O)C2=C
-
Structure Classification
-
Initial Source
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 10 mg/mL (33.28 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (292 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 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 |