1. Metabolic Enzyme/Protease PI3K/Akt/mTOR Epigenetics
  2. 11β-HSD AMPK
  3. 11β-HSD1-IN-25

11β-HSD1-IN-25 是一种选择性且口服有效的 11β-HSD1 抑制剂。 11β-HSD1-IN-25 能有效降低体外及血清中的糖皮质激素水平,并在体外和体内模型中减少脂质积累。11β-HSD1-IN-25 通过双重机制调节脂质代谢:抑制 11β-HSD1 以及激活 AMP 活化蛋白激酶 (AMPK) 信号通路。11β-HSD1-IN-25 可用于体内肥胖及相关代谢紊乱的研究。

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11β-HSD1-IN-25

11β-HSD1-IN-25 Chemical Structure

CAS No. : 1261266-23-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

11β-HSD1-IN-25 is a selective and orally active 11β-HSD1 inhibitor. 11β-HSD1-IN-25 effectively reduces glucocorticoid levels in vitro and serum, and diminishes lipid accumulation in both vitro and vivo. 11β-HSD1-IN-25 modulates lipid metabolism through dual mechanisms: inhibition of 11β-HSD1 and activation of the AMP-activated protein kinase (AMPK) signaling pathway. 11β-HSD1-IN-25 can be used for obesity and related metabolic disorders research[1].

体外研究
(In Vitro)

11β-HSD1-IN-25 (10 μM) 通过抑制 11β-HSD1 改善脂质代谢紊乱,并减少 3T3-L1 脂肪细胞中的脂质积累[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

11β-HSD1-IN-25 (0.5 mg/kg,口服,每日一次,持续 60 天) 可减轻肥胖,减少脂肪组织中脂肪细胞的大小,并通过抑制 11β-HSD1 来改善脂肪组织的脂质代谢紊乱,改善 11β-HSD1 慢病毒诱导 (或不诱导) 的雄性 C57BL/6 小鼠的脂肪细胞肥大和炎症[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 11β-HSD1 lentivirus induced (or not) (i.v.)-male C57BL/6 mice (8 weeks, 20-22 g)[1]
Dosage: 0.5 mg/kg
Administration: p.o., daily for 60 days
Result: Significantly mitigated weight gain when induced by 11β-HSD1 lentivirus.
Significantly reduced serum concentrations of corticosterone (CORT), cholesterol (CHO), triglycerides (TG), low-density lipoprotein (LDL), and high density lipoprotein (HDL).
Improved adipocyte morphology.
Decreased 11β-HSD1 protein expression.
Exhibited a substantial increase in the protein expression levels of UCP1, the p-AMPK/AMPK ratio, and CPT1 when reduced by 11β-HSD1 lentivirus when reduced by 11β-HSD1 lentivirus.
Showed a significant reduction in the mRNA expression of Hsd11b1, Srebp1c, Fas, and Acc1 and exhibited a increase in the expression levels of Cpt1, Ucp1, and Hsl when reduced by 11β-HSD1 lentivirus.
Not exhibited a significant elevation in FAS protein expression in adipose tissue when not reduced by 11β-HSD1 lentivirus.
Resulted in a substantial reduction in FAS protein expression.
Upregulated HSL protein no matter reduced by 11β-HSD1 lentivirus or not.
Significantly reduced F4/80 protein expression in adipose tissue.
分子量

432.31

Formula

C21H12F8O

CAS 号
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.

纯度 & 产品资料
参考文献
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产品名称:
11β-HSD1-IN-25
目录号:
HY-180549
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