Larsucosterol trimethylamine
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 97.0%
- Formula: C27H46O5S.0.45C3H9N
- Molecular Weight:509.32
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Macrophages
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Concentration:0, 5, 10, 15, 20, and 25 μM
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Incubation Time:48 hours
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Result:Induces cell proliferation and relative cell number after treatment for 48 h were 120% at 25 μM.
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Cell Line:Macrophages
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Concentration:0, 10, 20, 30, 40 and 50 μM
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Incubation Time:48 hours
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Result:Did not significantly affect the numbers of apoptotic or live cells.
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Cell Line:HepG2 cells
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Concentration:0, 3, 6, 12, and 25 μM
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Incubation Time:6 hours
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Result:Inhibited the activation of SREBP-1 and SREBP-2, and subsequently inhibit the expression HMG-CoA reductase.
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Cell Line:Macrophages
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Concentration:0, 3, 6, 12, and 25 μM
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Incubation Time:48 hours
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Result:Decreased LXRα levels in the nuclei in a does-dependent manner.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model[3]
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Dosage:25 mg/kg
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Administration:Intraperitoneal injection; twice in 14 hours
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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.
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Animal Model:Female C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model[3]
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Dosage:25 mg/kg
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Administration:Intraperitoneal injection; once every 3 days for 6 weeks
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Result:Decreased plasma cholesterol levels.
Reduced serum alkaline phosphatase, ALT, and AST levels.
Chemical Information
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Appearance Solid
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Molecular Weight 509.32
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Formula C27H46O5S.0.45C3H9N
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Color Off-white to yellow
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SMILES
C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCCC(C)(O)C)([H])[C@@]3([H])[C@@](CC1)([H])[C@@]4(C(C[C@H](CC4)OS(=O)(O)=O)=CC3)C.CN(C)C.[0.45]
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Synonyms
DUR-928 trimethylamine
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 33.33 mg/mL (65.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9634 mL | 9.8170 mL | 19.6340 mL | 49.0851 mL |
| 5 mM | 0.3927 mL | 1.9634 mL | 3.9268 mL | 9.8170 mL | |
| 10 mM | 0.1963 mL | 0.9817 mL | 1.9634 mL | 4.9085 mL | |
| 15 mM | 0.1309 mL | 0.6545 mL | 1.3089 mL | 3.2723 mL | |
| 20 mM | 0.0982 mL | 0.4909 mL | 0.9817 mL | 2.4543 mL | |
| 25 mM | 0.0785 mL | 0.3927 mL | 0.7854 mL | 1.9634 mL | |
| 30 mM | 0.0654 mL | 0.3272 mL | 0.6545 mL | 1.6362 mL | |
| 40 mM | 0.0491 mL | 0.2454 mL | 0.4909 mL | 1.2271 mL | |
| 50 mM | 0.0393 mL | 0.1963 mL | 0.3927 mL | 0.9817 mL | |
| 60 mM | 0.0327 mL | 0.1636 mL | 0.3272 mL | 0.8181 mL |
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