产品
编 号：F065044
分子式：C20H28O2
分子量：300.44
分子式：C20H28O2
分子量：300.44
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CAS No: 119188-33-9
产品详情
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.
体内研究：
Coronarin A (30 or 100 mg/kg; i.p. or p.o.; once daily for 22 days) ameliorates hyperglycemia in mice.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.Pharmacokinetic properties of Coronarin A after single administrationa in ob/ob mice.Coronarin At1/2 (h) tmax (h) Cmax (ng/mL) AUC0-t (ng?h/mL) AUC0-∞ (ng?h/mL) MRT (h)
i.p.14.81.0107345711104521.7
p.o.3.011.0388169418564.88
Data are presented as the mean of three mice. aCoronarin A was intraperitoneally or orally administered at 30 mg/kg to ob/ob mice.Animal Model:Male ob/ob mice
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
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.
体外研究：
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.Coronarin A (1-30 μM; 4 h) increases tyrosine phosphorylation of IRS1 through inhibiting mTOR/S6K1 signaling.
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.
体内研究：
Coronarin A (30 or 100 mg/kg; i.p. or p.o.; once daily for 22 days) ameliorates hyperglycemia in mice.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.Pharmacokinetic properties of Coronarin A after single administrationa in ob/ob mice.Coronarin At1/2 (h) tmax (h) Cmax (ng/mL) AUC0-t (ng?h/mL) AUC0-∞ (ng?h/mL) MRT (h)
i.p.14.81.0107345711104521.7
p.o.3.011.0388169418564.88
Data are presented as the mean of three mice. aCoronarin A was intraperitoneally or orally administered at 30 mg/kg to ob/ob mice.Animal Model:Male ob/ob mice
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
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.
体外研究：
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.Coronarin A (1-30 μM; 4 h) increases tyrosine phosphorylation of IRS1 through inhibiting mTOR/S6K1 signaling.
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