FXR agonist 18
FXR agonist 18 is an orally active FXR agonist, with an EC50 of 10 nM against human FXR and an EC50 of 1360 nM against human TGR5. FXR agonist 18 inhibits inflammatory responses by reducing nitrite production, downregulating the expression of pro-inflammatory genes (Tnf, Adgre1, Cyp8b1, upregulating the expression of FXR, Hmox1, Nqo1, Nrf2, and enhancing antioxidant responses. FXR agonist 18 ameliorates liver fibrosis in mice, exhibits protective effects in mice with cholestatic liver injury, and shows anti-MASH efficacy. FXR agonist 18 can be used in studies of metabolic dysfunction-associated steatohepatitis.
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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: 3061938-00-6
- 分子式: C27H44N2O3S
- 分子量:476.71
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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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
NQO1 |
体外実験
FXR agonist 18 (Compound 27) potently activates FXR-mediated transcription in HEK-293 cells, with an EC50 of 128 nM[1].
FXR agonist 18 acts as a partial agonist of human MRGPRX4, with an EC50 value of 25,685 nM[1].
FXR agonist 18 (20 μM; 1 h pretreatment, 24 h LPS stimulation) inhibits LPS (HY-D1056)-induced inflammatory responses in RAW264.7 macrophages by reducing nitrite production, downregulating the expression of pro-inflammatory genes (Tnf, Adgre1, Cyp8b1), upregulating the expression of FXR, Hmox1, Nqo1, and Nrf2, and enhancing antioxidant responses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
体内実験
FXR agonist 18 (20 mg/kg; p.o.; once daily; for 5 consecutive days) exerts significant protective effects in mice with ANIT (HY-W540630)-induced cholestatic liver injury by normalizing serum biomarkers and alleviating hepatocellular damage[1].
At a dose of 20 mg/kg, FXR agonist 18 (10-20 mg/kg; p.o.; daily; 4 weeks) improves histopathological, fibrotic and serum biomarker parameters in a metabolic dysfunction-associated steatohepatitis (MASH) model induced by the combination of Western diet (WD) and CCl4; the 10 mg/kg dose also exhibits significant anti-MASH efficacy[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (8-week-old male, CCl4-induced liver fibrosis)[1]
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Dosage:30 mg/kg
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Administration:p.o.; daily; 4 weeks
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Result:Markedly attenuated fibrotic pathology, including thinner collagen septa with reduced bridging architecture in portal regions.
Significantly reduced collagen deposition confirmed by Sirius red quantification.
Significantly reduced total liver collagen content compared to the OCA group.
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Animal Model:C57BL/6J (8-week-old male, ANIT-induced cholestatic liver injury)[1]
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Dosage:20 mg/kg
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Administration:p.o.; daily; 5 days
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Result:Effectively normalized all measured serum biomarkers (ALT, AST, ALP, TBA, TBIL) to levels comparable to normal controls.
Showed near-normal liver histology with minimal necrosis or inflammation.
Significantly reduced histopathological injury scores compared to the ANIT model group.
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Animal Model:C57BL/6J (8-week-old male, WD- and CCl4-coinduced metabolic dysfunction-associated steatohepatitis)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:p.o.; daily; 4 weeks
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Result:At 20 mg/kg: Significantly reduced inguinal and epididymal adipose tissue-to-body weight ratios to normal levels.
Achieved more pronounced reduction in hepatic lipid accumulation than OCA.
Significantly improved hepatocyte ballooning (surpassing OCA efficacy).
Achieved >50% reduction in fibrotic collagen area ratio (greater than OCA's 30% reduction).
Markedly ameliorated mitochondrial ultrastructural injuries.
Showed the most substantial improvements in serum biomarkers (ALT, AST, TBA, TC, HDL, LDL) compared to OCA.
At 10 mg/kg: Ameliorated hepatic steatosis and lobular inflammation.
Attenuated liver fibrosis.
化学情報
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CAS 番号 3061938-00-6
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分子量 476.71
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分子式 C27H44N2O3S
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SMILES
[H][C@@]12C[C@@H](CC[C@@]1([C@]3(CC[C@@]4([C@H](CC[C@]4([C@@]3([C@@H]([C@@H]2CC)O)[H])[H])[C@@H](CCC5=NNC(O5)=S)C)C)[H])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)
FXR agonist 18 関連分類
HY-183692 関連分類
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