Lapaquistat
CAS No. 189060-13-7
Lapaquistat( TAK475 | TAK 475 | Lapaquistat acetate )
Catalog No. M12962 CAS No. 189060-13-7
A novel potent, competitive, orally active squalene synthase inhibitor with IC50 of 78 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 312 | In Stock |
|
| 10MG | 467 | In Stock |
|
| 25MG | 748 | In Stock |
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| 100MG | Get Quote | In Stock |
|
| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameLapaquistat
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NoteResearch use only, not for human use.
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Brief DescriptionA novel potent, competitive, orally active squalene synthase inhibitor with IC50 of 78 nM.
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DescriptionA novel potent, competitive, orally active squalene synthase inhibitor with IC50 of 78 nM; displays no effect on plasma aspartate aminotransferase and alanine aminotransferase activities; effectively inhibits cholesterol synthesis in rat liver with ED50 of 2.9 mg/kg (p.o.), lowers plasma total cholesterol, triglyceride and phospholipid levels in rabbits, also inhibits the secretion of cholesterol, triglyceride and phospholipid components of very-low-density lipoprotein (VLDL) from liver.Dyslipidemia Phase 3 Discontinued.
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In Vitro——
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In VivoAnimal Model:Male WHHLMI rabbits, aged 2 months Dosage:100 or 200?mg/kg Administration:Diet supplemented; 100 or 200?mg/kg; 32 weeks Result:Increased collagen concentration and transformed coronary plaques into fibromuscular plaques.Suppressed the expression of MMP-1 and PAI-1 in the plaque and increased peripheral coenzyme Q10 levels.
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SynonymsTAK475 | TAK 475 | Lapaquistat acetate
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PathwayOthers
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TargetOther Targets
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RecptorOther Targets
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Research AreaCardiovascular Disease
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IndicationDyslipidemia
Chemical Information
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CAS Number189060-13-7
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Formula Weight645.146
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Molecular FormulaC33H41ClN2O9
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Purity>98% (HPLC)
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Solubility——
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SMILESO=C(O)CC1CCN(C(C[C@H]2O[C@H](C3=CC=CC(OC)=C3OC)C4=CC(Cl)=CC=C4N(CC(C)(C)COC(C)=O)C2=O)=O)CC1
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Chemical Name1-{2-[(3R,5S)-1-(3-acetoxy-2,2-dimethylpropyl)-7-chloro-1,2,3,5-tetrahydro-2-oxo-5-(2,3-dimethoxyphenyl)-4,1-benzoxazepine-3-yl] acetyl} piperidin-4-acetic acid
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Miki T, et al. J Med Chem. 2002 Sep 26;45(20):4571-80.
2. Amano Y, et al. Eur J Pharmacol. 2003 Apr 11;466(1-2):155-61.
3. Nishimoto T, et al. Br J Pharmacol. 2003 Jul;139(5):911-8.
4. Burnett JR. Curr Opin Investig Drugs. 2006 Sep;7(9):850-6.
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