| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Rasostrol (DUR-928; 0-25 μM; 8 h; HepG2 cells) ammonium salt inhibits cholesterol biosynthesis by reducing HMG-CoA reductase mRNA levels and reduces free [14C] cholesterol levels in a dose-dependent manner [1]. Rasostrol (0-25 μM; 6 h; HepG2 cells) ammonium salt inhibits HMG-CoA reductase expression by inhibiting the activation and expression of SREBP1 in hepatocytes [1]. Rasostrol (0-50 μM; 48 h) ammonium salt promotes macrophage proliferation and reduces its apoptosis [2]. Rasostrol (0-25 μM; 48 h; macrophages) ammonium salt inhibits the activation of hepatic oxosterol receptor LXRα [2].
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|---|---|
| ln Vivo |
Rasostrol (DUR-928; 25 mg/kg; intraperitoneal injection; twice every 14 hours; C57BL/6J mouse non-alcoholic fatty liver (NAFLD) model) ammonium reduced blood lipid levels in mice fed a high-fat diet [3]. Rasostrol (25 mg/kg; intraperitoneal injection; twice every 14 hours; C57BL/6J mouse non-alcoholic fatty liver (NAFLD) model) ammonium inhibited gene expression and suppressed ABCA1 expression. Rasostrol ammonium increased the levels of nuclear SREBP-1 protein and cytoplasmic FAS and ACC1 protein in liver tissue [3]. Rasostrol (25 mg/kg; intraperitoneal injection; once every 3 days for 6 weeks; C57BL/6J mouse non-alcoholic fatty liver (NAFLD) model) ammonium protected the liver from damage by inhibiting liver inflammation [3].
|
| Cell Assay |
Cell viability assay [2]
Cell Types: Macrophages Tested Concentrations: 0, 5, 10, 15, 20 and 25 μM Incubation Duration: 48 hours Experimental Results: After 48 hours of treatment with 25 μM, cell proliferation was induced, with a relative cell number of 120%. Apoptosis analysis [2] Cell Types: Macrophages Tested Concentrations: 0, 5, 10, 15, 20 and 25 μM Incubation Duration: 48 hours Experimental Results: No significant effect on the number of apoptotic or live cells. Western Blot Analysis [1] Cell Types: HepG2 cells Tested Concentrations: 0, 3, 6, 12 and 25 μM Incubation Duration: 6 hours Experimental Results: Inhibited the activation of SREBP-1 and SREBP-2, thereby inhibiting the expression of HMG-CoA reductase.
|
| Animal Protocol |
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. 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. |
| References |
|
| Molecular Formula |
C27H49NO5S
|
|---|---|
| Molecular Weight |
499.75
|
| CAS # |
2655654-16-1
|
| Appearance |
Typically exists as solids at room temperature
|
| 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.N
|
| Synonyms |
DUR-928 ammonium
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0010 mL | 10.0050 mL | 20.0100 mL | |
| 5 mM | 0.4002 mL | 2.0010 mL | 4.0020 mL | |
| 10 mM | 0.2001 mL | 1.0005 mL | 2.0010 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.
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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