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| ln Vitro |
Sarinsterol (12.5–200 μM; 24 h) did not reduce the viability of 3T3-L1 cells[1]. Sarinsterol (50–200 μM; 8 h) dose-dependently inhibited the accumulation of lipids and triglycerides in 3T3-L1 preadipocytes, reducing the accumulation to 26.6% of that in control differentiated cells at 200 μM[1]. Sarinsterol (50–200 μM; 24 h) dose-dependently increased the release of glycerol from 3T3-L1 adipocytes, with a statistically significant increase at 200 μM[1]. Sarinsterol (100–200 μM; 8 h) significantly reduced the mRNA and protein expression of PPARγ and C/EBPα in 3T3-L1 cells[1]. Salinsterol (100-200 μM; 8 days) significantly reduced the mRNA expression of adipogenesis marker genes (aP2, adiponectin, resistin, and FAS) in 3T3-L1 cells [1]. Salinsterol (20 μM; 24 hours) increased the mRNA expression of LXR-regulated cholesterol transport/uptake genes (ABCA1, ABCG1, and IDOL) and reduced cellular cholesterol content in foam cells derived from RAW264.7 macrophages [2]. Salinsterol has anti-tuberculosis activity with a MIC of 0.25 μg/mL [3]. Salinsterol showed no significant toxicity to Vero cells with an IC50 greater than 128 μg/mL [3].
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| ln Vivo |
Salinsterol (50 mg/kg; orally; daily; for 2 weeks) reduced atherosclerotic plaque burden in ApoE−/− mice, improved serum and liver lipid profiles, and regulated LXR-regulated cholesterol metabolism genes without inducing hepatic lipogenesis [2]. Salinsterol (10–30 mg/kg; intraperitoneal injection, single dose, administered 30 minutes before the test; 30 mg/kg; orally, once daily for 7 days) produced significant dose-dependent antidepressant-like effects in a mouse behavioral despair model [4].
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| Cell Assay |
Real-time quantitative PCR[1]
Cell Types: MDI-induced 3T3-L1 cells Tested Concentrations: 100, 200 μM Incubation Duration: 8 days (from the start of differentiation) Experimental Results: Significantly inhibited the mRNA expression of PPARγ and C/EBPα, both concentrations showed statistically significant inhibitory effects. Significantly inhibited the mRNA expression of aP2, adiponectin, resistin and FAS, both concentrations showed statistically significant inhibitory effects. Western Blot analysis [1] Cell Types: MDI-induced 3T3-L1 cells Tested Concentrations: 100, 200 μM Incubation Duration: 8 days (from the start of differentiation) Experimental Results: Significantly inhibited the protein expression of PPARγ and C/EBPα, both concentrations showed statistically significant inhibitory effects. |
| Animal Protocol |
Animal/Disease Models:ApoE−/− mice (8 weeks old) fed a high-fat diet [2]
Doses: 50 mg/kg Route of Administration: Oral; daily; for 2 weeks Experimental Results: The atherosclerotic plaque burden was reduced, and the aortic plaque area (percentage of total aortic area) and the aortic root cross-sectional plaque area were significantly lower than those of the control mice. Serum total cholesterol, low-density lipoprotein cholesterol and triglyceride levels were significantly reduced; serum high-density lipoprotein cholesterol levels were significantly increased. There was no significant change in liver total cholesterol levels; liver triglyceride levels were significantly lower than those of the control mice. Hepatic steatosis was reduced, and liver weight and liver weight/body weight ratio were lower than those of the control mice; liver adipogenesis genes (SREBP-1c, ACC, FASN, SCD1, chREBP) were not upregulated. The mRNA levels of cholesterol efflux transporters ABCA1 and ABCG1 and LDLR degradation protein IDOL in peritoneal macrophages were upregulated. The mRNA levels of cholesterol-degrading enzyme CYP7A1, cholesterol efflux transporters ABCG5 and ABCG8, and HDL cholesterol influx receptor SR-B1 were upregulated in the liver. The mRNA level of cholesterol absorption transporter NPC1L1 was downregulated in the intestine; the mRNA levels of cholesterol efflux transporters ABCG5, ABCG8, and ABCA1 were upregulated in the intestine. Animal/Disease Models:ICR (male, 20-22 g) [4] Doses: 10 mg/kg; 20 mg/kg; 30 mg/kg (single dose; behavioral test); 30 mg/kg (neurotransmitter analysis) Route of Administration: Intraperitoneal injection (10-30 mg/kg); oral administration; once daily for 7 days (30 mg/kg) Experimental Results: Reduced immobility time in forced swimming and tail suspension tests. No significant changes in motor activity in open field tests at all tested doses. Increased brain levels of serotonin (5-HT), 5-hydroxyindoleacetic acid (5-HIAA), and norepinephrine (NE). No significant effect on brain dopamine (DA) levels. |
| References |
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| Molecular Formula |
C29H48O2
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|---|---|
| Molecular Weight |
428.69
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| CAS # |
6901-60-6
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| Appearance |
White to off-white solid
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| SMILES |
C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCC(C=C)(O)C(C)C)([H])[C@@]3([H])[C@@](CC1)([H])[C@@]4(C(C[C@H](CC4)O)=CC3)C
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| 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)
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| 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 | 2.3327 mL | 11.6634 mL | 23.3269 mL | |
| 5 mM | 0.4665 mL | 2.3327 mL | 4.6654 mL | |
| 10 mM | 0.2333 mL | 1.1663 mL | 2.3327 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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