AMPK/mTOR modulator-1
AMPK/mTOR modulator-1, Ginsenoside derivative, is an orally active mTOR inhibitor and AMPK activator. AMPK/mTOR modulator-1 activates AMPK signaling with a Kd of 4.759 μM. AMPK/mTOR modulator-1 promotes M1-like tumor-associated macrophage polarization while suppressing M2-like polarization. AMPK/mTOR modulator-1 can enhance glycolysis. AMPK/mTOR modulator-1 significantly inhibits tumor progression and shows anti-inflammation activity. AMPK/mTOR modulator-1 can be used for the research of colorectal cancer.
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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。
- CAS 番号: 1190602-80-2
- 分子式: C31H56O4
- 分子量:492.77
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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- 純度とドキュメンテーション
- 参考文献
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生物活性
製品説明
IC50 & Target
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AMPK 4.759 μM (Kd) |
体外実験
AMPK/mTOR modulator-1 (Compound AD-1) directly binds to recombinant AMPK protein with a Kd of 4.759 × 10−6 M[1].
AMPK/mTOR modulator-1 (2.5-10 μM; 24 h) promotes M1-like polarization and suppresses M2-like polarization in RAW264.7-derived TAMs in a dose-dependent manner[1].
AMPK/mTOR modulator-1 (2.5-10 μM; 24 h) activates AMPK and inhibits mTOR signaling in RAW264.7-derived TAMs in a dose-dependent manner[1].
AMPK/mTOR modulator-1 (2.5-10 μM; 24 h) enhances glycolytic activity in RAW264.7-derived TAMs in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7-derived TAMs in TCS of mouse colon cancer cells (CT26)
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Concentration:2.5, 5, and 10 μM
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Incubation Time:24 h
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Result:Downregulated M2 -associated markers (Arg-1, IL-10, and TGF-β)
and upregulated M1-associated markers (iNOS, TNF-α, and IL-1β).
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Cell Line:RAW264.7-derived TAMs in TCS of mouse colon cancer cells (CT26)
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Concentration:2.5, 5, and 10 μM
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Incubation Time:24 h
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Result:Increased protein levels of iNOS and reduced Arg-1 levels.
Increased P-AMPK AMPK ratio and reduced p-mTOR/mTOR ratio.
Upregulated the expression of key glycolytic en-zymes, including GLUT1, LDHA, PKM2, and HK2.
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Cell Line:RAW264.7-derived TAMs in TCS of mouse colon cancer cells (CT26)
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Concentration:2.5, 5, and 10 μM
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Incubation Time:24 h
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Result:Reduced TGF-β, IL-10 levles and increased IL-1β, TNF-α levels.
体内実験
AMPK/mTOR modulator-1 (10 mg/kg; oral gavage; daily; 15 days) suppresses tumor growth and reprograms TAM polarization in HT-29 cells xenograft mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CAC mice induced by AOM/DSS (male, BALB/c， 6–8 weeks old, 20–22 g)[1]
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Dosage:10 mg/kg
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Administration:oral gavage; daily; 64 days
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Result:Restored colon length and reduced tumor number.
Alleviated crypt destruction, epithelial damage, and inflammatory infiltration.
Decreased Ki-67-positive proliferating cells and reduced proportion of F4/80+CD206+ (M2-like) TAMs.
Increased levels of TNF-α and IL-1β and decreased IL-10 levels.
Increased iNOS protein levels and decreased Arg-1 protein levels.
Increased infiltration of F4/80+CD86+ (M1-like) TAMs and decreased F4/80+CD206+ TAMs in colonic tissues.
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Animal Model:CRC mice with HT-29 cells xenograft (female, BALB/c nude, 6–8 weeks old, 20–22 g)[1]
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Dosage:10 mg/kg
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Administration:oral gavage; daily; 15 days
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Result:Reduced tumor volume and weight, inflammatory cell infiltration and improved tissue architecture in tumor sections.
Decreased tumor cell proliferation (lower Ki-67 expression).
Elevated iNOS expression and decreased Arg-1 expression.
Increased abundance of F4/80+CD86+ (M1-like) TAMs; reduced number of F4/80+CD206+ (M2-like) TAMs in tumor tissue.
化学情報
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CAS 番号 1190602-80-2
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分子量 492.77
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分子式 C31H56O4
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SMILES
CC1(C)[C@@H](O)CC[C@@]2(C)C1CC[C@]3(C)C2C[C@@H](O)C4[C@@]3(C)CCC4[C@](C)(OC)CCCC(C)(C)O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
AMPK/mTOR modulator-1 関連分類
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