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Larsucosterol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Larsucosterol图片
CAS NO:884905-07-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
DUR-928
产品介绍
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。
生物活性

Larsucosterol (DUR-928), acholesterolmetabolite, is a potentliver X receptor (LXR)antagonist. Larsucosterol as a potent endogenous regulator decreases lipogenesis. Larsucosterol inhibits thecholesterolbiosynthesis 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].

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].

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

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.