2. Metabolic Enzyme/Protease
  3. Endogenous Metabolite
  4. Larsucosterol

Larsucosterol (DUR-928) 是一种胆固醇代谢物，是一种有效的肝 X 受体 (LXR) 拮抗剂。Larsucosterol 是一种有效的内源性脂肪生成调节剂。Larsucosterol 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。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 Larsucosterol (trimethylamine) 通常具有更好的水溶性和稳定性。

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Larsucosterol Chemical Structure

Larsucosterol Chemical Structure

CAS No. : 884905-07-1

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Larsucosterol 的其他形式现货产品:

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Larsucosterol 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Larsucosterol (DUR-928), a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol as a potent endogenous regulator decreases lipogenesis. Larsucosterol 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) 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]。
拉苏甾醇 (0-25 μM；6 小时；HepG2 细胞) 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) 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) 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.

Larsucosterol 相关抗体:

Cell Proliferation 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)

拉苏甾醇 (DUR-928；25 mg/kg；腹腔注射；14 小时内给药两次；患有非酒精性脂肪性肝病 (NAFLD) 模型的 C57BL/6J 小鼠) 降低喂食高脂肪饮食的小鼠的血脂水平[3]。
拉苏甾醇 (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) 抑制基因表达并抑制 ABCA1 表达。Larsucosterolcreases nuclear SREBP-1 Protein levels和cytoplasmic FAS和ACC1 protein levels in liver tissue[3]。
Larsucosterol (25 mg/kg；腹腔注射；每 3 天一次，持续 6 周；C57BL /6J 非酒精性脂肪性肝病 (NAFLD) 小鼠模型) 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.
Clinical Trial
分子量

482.72

Formula

C27H46O5S
CAS 号
结构分类
初始来源
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

Larsucosterol 相关分类

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Keywords:

Larsucosterol884905-07-1DUR-928DUR928DUR 928Endogenous Metabolitecholesterol metabolitelipogenesismRNASREBP-1cholesterol biosynthesisHepG2 cellsmacrophagesInhibitorinhibitorinhibit

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