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Larsucosterol trimethylamine

Alias: DUR-928 trimethylamine
Cat No.:V138658 Purity: ≥98%
Larsucosterol trimethylamine is a cholesterol metabolite and a potent hepatic X receptor (LXR) antagonist.
Larsucosterol trimethylamine
Larsucosterol trimethylamine Chemical Structure Product category: Endogenous Metabolite
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
50mg
100mg
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Other Forms of Larsucosterol trimethylamine:

  • Larsucosterol (DUR-928)
  • Larsucosterol sodium (DUR-928 sodium)
  • Larsucosterol (trimethylamine) (DUR-928 (trimethylamine))
  • Larsucosterol ammonium
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Top Publications Citing lnvivochem Products
Product Description
Larsucosterol trimethylamine is a cholesterol metabolite and a potent hepatic receptor X (LXR) antagonist. As a potent endogenous regulator, larsucosterol trimethylamine reduces lipogenesis. It inhibits cholesterol biosynthesis by lowering mRNA levels and suppressing SREBP-1 activation.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Rasusterol (DUR-928; 0-25 μM; 8 h; HepG2 cells) trimethylamine inhibits cholesterol biosynthesis by reducing HMG-CoA reductase mRNA levels and reduces free [14C] cholesterol levels in a dose-dependent manner [1]. Rasusterol (0-25 μM; 6 h; HepG2 cells) trimethylamine inhibits HMG-CoA reductase expression by inhibiting the activation and expression of SREBP1 in hepatocytes [1]. Rasusterol (0-50 μM; 48 h) trimethylamine promotes macrophage proliferation and reduces apoptosis [2]. Rasusterol (0-25 μM; 48 h; macrophages) trimethylamine inhibits the activation of hepatic oxosterol receptor LXRα [2].
ln Vivo
Rasusterol (DUR-928; 25 mg/kg; intraperitoneal injection; twice every 14 hours; C57BL/6J mouse non-alcoholic fatty liver (NAFLD) model) Trimethylamine can reduce blood lipid levels in mice fed a high-fat diet [3]. Rasusterol (25 mg/kg; intraperitoneal injection; twice every 14 hours; C57BL/6J mouse non-alcoholic fatty liver (NAFLD) model) Trimethylamine can inhibit gene expression and inhibit ABCA1 expression. Rasusterol can increase the level of nuclear SREBP-1 protein and cytoplasmic FAS and ACC1 protein in liver tissue [3]. Rasusterol (25 mg/kg; intraperitoneal injection; once every 3 days for 6 weeks; C57BL/6J mouse non-alcoholic fatty liver (NAFLD) model) Trimethylamine can protect the liver from damage by inhibiting liver inflammation [3].
Animal Protocol
Animal/Disease Models:Female C57BL/6J mice with non-alcoholic fatty liver disease (NAFLD) [3]
Doses: 25 mg/kg<
Route of Administration:Intraperitoneal injection; twice every 14 hours
Experimental Results:Plasma triglycerides (TG), total cholesterol (CHOL), and high-density lipoprotein cholesterol (HDL-C) decreased by 40%, 15%, and 20%, respectively. The mRNA levels of SREBP-1c, ACC1, and FAS decreased by 46%, 57%, and 49%, respectively. ABCA1 expression was inhibited. The levels of nuclear SREBP-1, cytoplasmic ACC1, and FAS proteins decreased by 74%, 58%, and 47%, respectively.
Animal/Disease Models:Female C57BL/6J mice, non-alcoholic fatty liver disease (NAFLD) model [3]
Doses: 25 mg/kg
Route of Administration: Intraperitoneal injection; once every 3 days for 6 weeks
Experimental Results: Decreased plasma cholesterol levels. Decreased serum alkaline phosphatase, ALT and AST levels.
References

[1]. Sulfated oxysterol, 25HC3S, is a potent regulator of lipid metabolism in human hepatocytes. Biochem Biophys Res Commun. 2007 Sep 7;360(4):802-8.

[2]. 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.

[3]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H46O5S.0.45C3H9N
Molecular Weight
509.32
Related CAS #
Larsucosterol; Larsucosterol sodium; Larsucosterol ammonium; 2655654-16-1
Appearance
Off-white to yellow solid
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]
Synonyms
DUR-928 trimethylamine
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: 请将本产品存放在密封保护的环境中,避免受潮。
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~33.33 mg/mL (~65.44 mM; with sonication)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (4.91 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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