Larsucosterol (trimethylamine) (Synonyms: DUR-928 (trimethylamine)) |
Katalog-Nr.GC65936
One-Click Copy Product Info
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Larsucosterol (DUR-928) Trimethylamin, ein Cholesterinmetabolit, ist ein potenter Antagonist des Leber-X-Rezeptors (LXR). Larsucosteroltrimethylamin als potenter endogener Regulator verringert die Lipogenese. Larsucosterol-Trimethylamin hemmt die Cholesterinbiosynthese, indem es die mRNA-Spiegel senkt und die Aktivierung von SREBP-1 hemmt.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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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 | ||
| Überlieferungen | DUR-928 (trimethylamine) | ||
| Formula | C30H46O5S.0.45C3H9N | M.Wt | 509.32 |
| Löslichkeit | DMSO : 33.33 mg/mL (65.44 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9634 mL | 9.817 mL | 19.634 mL |
| 5 mM | 392.7 μL | 1.9634 mL | 3.9268 mL |
| 10 mM | 196.3 μL | 981.7 μL | 1.9634 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)