1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. LXR Endogenous Metabolite
  3. Larsucosterol ammonium

Larsucosterol ammonium  (Synonyms: DUR-928 ammonium)

目录号: HY-139576C
产品使用指南 技术支持

Larsucosterol (DUR-928) ammonium 是一种胆固醇代谢物,是一种有效的肝 X 受体 (LXR) 拮抗剂。Larsucosterol ammonium 是一种有效的内源性脂肪生成调节剂。Larsucosterol ammonium 通过降低 mRNA 水平和抑制 SREBP-1 的激活抑制胆固醇的生物合成。

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Larsucosterol ammonium Chemical Structure

Larsucosterol ammonium Chemical Structure

CAS No. : 2655654-16-1

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Larsucosterol ammonium 的其他形式现货产品:

Other Forms of Larsucosterol ammonium:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Larsucosterol (DUR-928) ammonium, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol ammonium as a potent endogenous regulator decreases lipogenesis. Larsucosterol ammonium inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1[1][2][3].

体外研究
(In Vitro)

Larsucosterol (DUR-928;0-25 μM;8 小时;HepG2 细胞) ammonium 通过降低 HMG-CoA 还原酶 mRNA 水平来抑制胆固醇生物合成,并以剂量依赖的方式降低游离 [14C] 胆固醇[1]
Larsucosterol (0-25 μM;6 小时;HepG2 细胞) ammonium 通过抑制肝细胞中 SREBP1 的激活和表达来抑制 HMG-CoA 还原酶的表达[1]
Larsucosterol (0-50 μM;48 h) ammonium 在巨噬细胞中增加细胞增殖并减少细胞凋亡[2]
Larsucosterol (0-25 μM;48 h;巨噬细胞) ammonium 抑制肝氧甾醇受体 LXRα 的激活[2]

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

Cell Viability Assay[2]

Cell Line: Macrophages
Concentration: 0, 5, 10, 15, 20, and 25 μM
Incubation Time: 48 hours
Result: Induces cell proliferation and relative cell number after treatment for 48 h were 120% at 25 μM.

Apoptosis Analysis[2]

Cell Line: Macrophages
Concentration: 0, 5, 10, 15, 20, and 25 μM
Incubation Time: 48 hours
Result: Did not significantly affect the numbers of apoptotic or live cells.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0, 3, 6, 12, and 25 μM
Incubation Time: 6 hours
Result: Inhibited the activation of SREBP-1 and SREBP-2, and subsequently inhibit the expression HMG-CoA reductase.

Western Blot Analysis[2]

Cell Line: Macrophages
Concentration: 0, 3, 6, 12, and 25 μM
Incubation Time: 48 hours
Result: Decreased LXRα levels in the nuclei in a does-dependent manner.
体内研究
(In Vivo)

Larsucosterol (DUR-928;25 mg/kg;腹腔注射;14小时内两次;患有非酒精性脂肪性肝病 (NAFLD) 模型的 C57BL/6J 小鼠) ammonium 可降低高脂饮食喂养小鼠的血清脂质水平[3]
Larsucosterol (25 mg/kg;腹腔注射;14 小时内两次;患有非酒精性脂肪性肝病 (NAFLD) 模型的 C57BL/6J 小鼠) ammonium 可抑制上述基因的表达,并抑制 ABCA1 的表达。Larsucosterol ammonium 可提高肝组织中细胞核 SREBP-1 蛋白水平以及细胞质 FAS 和 ACC1 蛋白水平[3]
Larsucosterol (25 mg/kg;腹腔注射;每 3 天一次,持续 6 周;非酒精性脂肪性肝病 (NAFLD) 模型 C57BL/6J 小鼠) ammonium 通过抑制肝脏炎症来保护肝脏免受损伤[3]

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

Animal Model: Female C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model[3]
Dosage: 25 mg/kg
Administration: Intraperitoneal injection; once every 3 days for 6 weeks
Result: Decreased plasma cholesterol levels.
Reduced serum alkaline phosphatase, ALT, and AST levels.
Animal Model: Female C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model[3]
Dosage: 25 mg/kg
Administration: Intraperitoneal injection; twice in 14 hours
Result: Decreased plasma TG, CHOL, and HDL-C by 40, 15, and 20%, respectively.
Reduced the mRNA levels of SREBP-1c, ACC1, and FAS by 46, 57, and 49%, respectively.
Suppressed ABCA1 expression.
Suppressed nuclear SREBP-1, cytoplasmic ACC1, and FAS protein levels by 74, 58, and 47%, respectively.
分子量

499.75

同用名

DUR-928 ammonium

Formula

C27H49NO5S

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
  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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