Larsucosterol sodium
Larsucosterol (DUR-928) sodium, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol sodium as a potent endogenous regulator decreases lipogenesis. Larsucosterol sodium inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.
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- CAS. Nr.: 1174047-40-5
- Formel: C27H45NaO5S
- Molecular Weight:504.70
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Larsucosterol (DUR-928; 0-25 μM; 8 h; HepG2 cells) sodium 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) sodium inhibits HMG-CoA reductase expression by inhibition of both SREBP1 activation and expression in hepatocytes[1].
Larsucosterol (0-50 μM; 48 h) sodium increases cell proliferation and decreases apoptosis in macrophages[2].
Larsucosterol (0-25 μM; 48 h; macrophages) sodium 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) sodium 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) sodium 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1174047-40-5
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Molecular Weight 504.70
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Formel C27H45NaO5S
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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[Na])=O)=CC3)C
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Synonyms
DUR-928 sodium
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Larsucosterol sodium Related Classifications
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