Larsucosterol (trimethylamine) DUR-928 (trimethylamine)|西域试剂

Larsucosterol (trimethylamine) DUR-928 (trimethylamine),98.0%

产品编号：Bellancom-139576B| 分子式：C₃₀H₄₆O₅S.0.45C₃H₉N| 分子量：509.32

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货号	价格	库存与货期
Bellancom-139576B	￥3500.00	杭州北京（现货）
Bellancom-139576B	￥6000.00	杭州北京（现货）
Bellancom-139576B	￥12500.00	杭州北京（现货）

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Larsucosterol (trimethylamine) DUR-928 (trimethylamine)

产品介绍

Larsucosterol (DUR-928) trimethylamine 是一种胆固醇代谢物，是一种有效的肝 X 受体 (LXR) 拮抗剂。Larsucosterol trimethylamine 是一种有效的内源性脂肪生成调节剂。Larsucosterol trimethylamine 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) trimethylamine, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol trimethylamine as a potent endogenous regulator decreases lipogenesis. Larsucosterol trimethylamine inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.

体外研究

Larsucosterol (DUR-928; 0-25 μM; 8 h; HepG2 cells) trimethylamine inhibits cholesterol biosynthesis by decreasing HMG-CoA reductase mRNA levels and decreases free [¹⁴C] cholesterol in a dose-dependent manner.
Larsucosterol (0-25 μM; 6 h; HepG2 cells) trimethylamine inhibits HMG-CoA reductase expression by inhibition of both SREBP1 activation and expression in hepatocytes.
Larsucosterol (0-50 μM; 48 h) trimethylamine increases cell proliferation and decreases apoptosis in macrophages.
Larsucosterol (0-25 μM; 48 h; macrophages) trimethylamine inhibits activation of liver oxysterol receptor LXRα.

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

Cell Proliferation Assay

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

Cell Line:	Macrophages
Concentration:	0, 10, 20, 30, 40 and 50 μM
Incubation Time:	48 hours
Result:	Did not significantly affect the numbers of apoptotic or live cells.

Western Blot Analysis

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

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) trimethylamine reduces serum lipid levels in mice fed a high-fat diet.
Larsucosterol (25 mg/kg; i.p.; twice in 14 hours; C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model) trimethylamine 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.
Larsucosterol (25 mg/kg; i.p.; once every 3 days for 6 weeks; C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model) trimethylamine protects the liver from injury by suppressing hepatic inflammation.

西域 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
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.

Animal Model:	Female C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model
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.

体内研究

西域 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
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.

Animal Model:	Female C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model
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.

体内研究

西域 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
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.

Animal Model:	Female C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (65.44 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9634 mL	9.8170 mL	19.6340 mL
5 mM	0.3927 mL	1.9634 mL	3.9268 mL
10 mM	0.1963 mL	0.9817 mL	1.9634 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式