Larsucosterol (trimethylamine)
(Synonyms: DUR-928 (trimethylamine)) 目录号 : GC65936
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。
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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[1][2][3].
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[1].
Larsucosterol (0-25 μM; 6 h; HepG2 cells) trimethylamine inhibits HMG-CoA reductase expression by inhibition of both SREBP1 activation and expression in hepatocytes[1].
Larsucosterol (0-50 μM; 48 h) trimethylamine increases cell proliferation and decreases apoptosis in macrophages[2].
Larsucosterol (0-25 μM; 48 h; macrophages) trimethylamine 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, 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[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. |
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[3].
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[3].
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[3].
| 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. |
| 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. |
| Cas No. | SDF | Download SDF | |
| 别名 | DUR-928 (trimethylamine) | ||
| 分子式 | C30H46O5S.0.45C3H9N | 分子量 | 509.32 |
| 溶解度 | DMSO : 33.33 mg/mL (65.44 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9634 mL | 9.817 mL | 19.634 mL |
| 5 mM | 0.3927 mL | 1.9634 mL | 3.9268 mL |
| 10 mM | 0.1963 mL | 0.9817 mL | 1.9634 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。