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Larsucosterol (Synonyms: DUR-928)

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Larsucosterol  (Synonyms: DUR-928)

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。

Larsucosterol (Synonyms: DUR-928)

Larsucosterol Chemical Structure

CAS No. : 884905-07-1

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Larsucosterol 的其他形式现货产品:

Larsucosterol (trimethylamine)

Larsucosterol 相关产品

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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 h; HepG2 cells) inhibits cholesterol biosynthesis by decreasing HMG-CoA reductase mRNA levels and decreases free [14C] cholesterol in a dose-dependent manner[1].
Larsucosterol (0-25 μM; 6 h; HepG2 cells) inhibits HMG-CoA reductase expression by inhibition of both SREBP1 activation and expression in hepatocytes[1].
Larsucosterol (0-50 μM; 48 h) increases cell proliferation and decreases apoptosis in macrophages[2].
Larsucosterol (0-25 μM; 48 h; macrophages) inhibits activation of liver oxysterol receptor LXRα[2].

Shanghai Jinpan Biotech Co Ltd 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)

Larsucosterol (DUR-928; 25 mg/kg; i.p.; twice in 14 hours; C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model) reduces serum lipid levels in mice fed a high-fat diet[3].
Larsucosterol (25 mg/kg; i.p.; twice in 14 hours; C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model) suppressed the expression of the genes and inhibits ABCA1 expressionde. Larsucosterolcreases nuclear SREBP-1 Protein levels and cytoplasmic FAS and ACC1 protein levels in liver tissue[3].
Larsucosterol (25 mg/kg; i.p.; once every 3 days for 6 weeks; C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model) protects the liver from injury by suppressing hepatic inflammation[3].

Shanghai Jinpan Biotech Co Ltd 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

884905-07-1
结构分类
  • Steroids
初始来源
  • 内源性代谢物
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
Data Sheet (534 KB) 产品使用指南 (1538 KB)

参考文献

  • [1]. Ren S, et, al. Sulfated oxysterol, 25HC3S, is a potent regulator of lipid metabolism in human hepatocytes. Biochem Biophys Res Commun. 2007 Sep 7;360(4):802-8.  [Content Brief]

    [2]. Ma Y, et, al. 25-Hydroxycholesterol-3-sulfate regulates macrophage lipid metabolism via the LXR/SREBP-1 signaling pathway. Am J Physiol Endocrinol Metab. 2008 Dec;295(6):E1369-79.  [Content Brief]

    [3]. Xu L, et, al. 5-cholesten-3β,25-diol 3-sulfate decreases lipid accumulation in diet-induced nonalcoholic fatty liver disease mouse model. Mol Pharmacol. 2013 Mar;83(3):648-58.  [Content Brief]

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