| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Larsucosterol (DUR-928; 0-25 μM; 8 h; HepG2 cells) reduces free [14C] cholesterol in a dose-dependent manner and inhibits the manufacture of cholesterol via lowering HMG-CoA reductase mRNA levels[1]. HepG2 cells exposed to levocosterol (0–25 μM) for 6 hours suppresses the expression of HMG-CoA reductase via blocking SREBP1 activation and expression in hepatocytes[1]. In macrophages, leuconosterol (0–50 μM; 48 h) promotes cell division and reduces apoptosis[2]. Liver oxysterol receptor LXRα activity is inhibited by leucosterol (0-25 μM; 48 h; macrophages)[2].
|
|---|---|
| ln Vivo |
Mice fed a high-fat diet have lower serum lipid levels when given lenucosterol (DUR-928; 25 mg/kg; ip; twice in 14 hours; C57BL/6J mice with nonalcoholic fatty liver disorders (NAFLD) model)[3]. Larsucosterol decreases the expression of ABCA1 and suppresses the expression of other genes in C57BL/6J mice with nonalcoholic fatty liver disease (NAFLD) model (25 mg/kg; ip; twice in 14 hours). In liver tissue, levosucosterol reduces the amounts of cytoplasmic FAS and ACC1 proteins as well as nuclear SREBP-1 protein[3]. By reducing hepatic inflammation, levofosterol (25 mg/kg; ip; once every three days for six weeks; C57BL/6J mice with nonalcoholic fatty liver disorders (NAFLD) model) shields the liver from damage[3].
|
| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: Macrophages Tested Concentrations: 0, 5, 10, 15, 20, and 25 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induces cell proliferation and relative cell number after treatment for 48 h were 120% at 25 μM. Apoptosis Analysis[2] Cell Types: Macrophages Tested Concentrations: 0, 5, 10, 15, 20, and 25 μM Incubation Duration: 48 hrs (hours) Experimental Results: Did not Dramatically affect the numbers 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 hrs (hours) Experimental Results: Inhibited the activation of SREBP-1 and SREBP-2, and subsequently inhibit the expression HMG-CoA reductase. Western Blot Analysis[2] Cell Types: Macrophages Tested Concentrations: 0, 3, 6, 12, and 25 μM Incubation Duration: 48 hrs (hours) Experimental Results: diminished LXRα levels in the nuclei in a does-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Female C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model[3]
Doses: 25 mg/kg Route of Administration: intraperitoneal (ip) injection; once every 3 days for 6 weeks Experimental Results: diminished plasma cholesterol levels. decreased serum alkaline phosphatase, ALT, and AST levels. Animal/Disease Models: Female C57BL/6J mice with nonalcoholic fatty liver diseases (NAFLD) model[3] Doses: 25 mg/kg Route of Administration: intraperitoneal (ip) injection; twice in 14 hrs (hours) Experimental Results: diminished plasma TG, CHOL , and HDL-C by 40, 15, and 20%, respectively. decreased 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. |
| References |
|
| Molecular Formula |
C27H46O5S
|
|---|---|
| Molecular Weight |
482.72
|
| Exact Mass |
482.306
|
| CAS # |
884905-07-1
|
| Related CAS # |
Larsucosterol (trimethylamine);Larsucosterol sodium;1174047-40-5
|
| PubChem CID |
11583880
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.2±0.1 g/cm3
|
| Index of Refraction |
1.552
|
| LogP |
7.95
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
33
|
| Complexity |
858
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
S(=O)(=O)(O)O[C@H]1CC[C@@]2(C)C(C1)=CC[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)CCCC(C)(C)O)CC[C@H]21
|
| InChi Key |
PIUZYOCNZPYXOA-ZHHJOTBYSA-N
|
| InChi Code |
InChI=1S/C27H46O5S/c1-18(7-6-14-25(2,3)28)22-10-11-23-21-9-8-19-17-20(32-33(29,30)31)12-15-26(19,4)24(21)13-16-27(22,23)5/h8,18,20-24,28H,6-7,9-17H2,1-5H3,(H,29,30,31)/t18-,20+,21+,22-,23+,24+,26+,27-/m1/s1
|
| Chemical Name |
[(3S,8S,9S,10R,13R,14S,17R)-17-[(2R)-6-hydroxy-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl] hydrogen sulfate
|
| 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 |
| 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
|
|---|---|
| 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 | 2.0716 mL | 10.3580 mL | 20.7159 mL | |
| 5 mM | 0.4143 mL | 2.0716 mL | 4.1432 mL | |
| 10 mM | 0.2072 mL | 1.0358 mL | 2.0716 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
