FXR antagonist 1 (化合物 F6) 是一种口服有效的、选择性的肠道FXR拮抗剂 (IC50=2.1 μM)。FXR antagonist 1 通过拮抗肠道FXR和反馈激活肝脏FXR来选择性地抑制肠道FXR信号，改善 NASH (非酒精性脂肪性肝炎) 模型中的肝脏脂肪变性、炎症和纤维化。FXR antagonist 1 可用于 NASH 的研究。
| 生物活性 | FXRantagonist 1 (compound F6) is an orally active and selective intestinalFXRantagonist (IC50=2.1 μM).FXRantagonist 1 selectively inhibits intestinalFXRsignalling through antagonism of intestinalFXRand feedback activation of hepaticFXRto improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models.FXRantagonist 1 can be used in NASH studies[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | FXR antagonist 1 (0-100 μM; 24 h) shows FXR antagonistic activities in HEK293T cells[1].
Cell Viability Assay[1] | Cell Line: | HEK293T cells (co-transfected with pCMV-Script-hFXR and pGL4.11-hSHP-Luciferase) | | Concentration: | 0-100 μM | | Incubation Time: | 24 h | | Result: | Exhibited FXR antagonistic activities with an IC50value of 2.1 μM. |
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体内研究
(In Vivo) | FXR antagonist 1 (10 mg/kg; p.o.; single daily for 12 weeks) reduces adiposity and improves glucose sensitivity and ameliorates the progress of NASH in GAN-diet-induced NASH mice[1].
FXR antagonist 1 (10 mg/kg; p.o.; single daily for 12 weeks) inhibits intestinal FXR Signaling but indirectly activates hepatic FXR signaling in GAN-diet-induced mice[1].
FXR antagonist 1 (3, 10, 30 mg/kg; p.o.; single daily for 4 weeks) dose-dependently alleviates NASH pathologies in HFMCD-diet-induced mice[1].
| Animal Model: | Adult male C57BL/6 mice (GAN (Gubra-amylin NASH)-diet induced NASH model)[1]. | | Dosage: | 10 mg/kg | | Administration: | Oral administration; single daily for 12 weeks. | | Result: | Reversed metabolic dysfunction in GAN-induced NASH mice.
Reduced GAN-diet-induced hepatic steatosis, injury, inflammation, and fibrosis.
Inhibited the hepatic mRNA expression involved in lipid metabolism, inflammatory signaling, and fibrogenesis in GAN-diet-induced mice.
Significantly antagonized intestinal FXR signaling and bile acid reabsorption. |
| Animal Model: | Adult male C57BL/6 mice (HFMCD-diet induced NASH model)[1]. | | Dosage: | 3, 10, 30 mg/kg | | Administration: | Oral administration; single daily for 4 weeks. | | Result: | Significantly decreased serum ALT and AST levels at 30 mg/kg, and markedly lowered the hepatic TG concentration in both 10 and 30 mg/kg.
Lowered hepatic hydroxyproline level. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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