Atorvastatin_134523-00-5_DataSheet_MedChemExpress

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:Cholesterol is the major sterol in mammals, and its importance in fundamental cellular processes is becoming more appreciated.IC50 value:Target:In vitro: GT1–7 hypothalamic cells subjected to cholesterol depletion in vitro produced 20–31% reductions in cellular cholesterol content, similar to the decrease in cholesterol synthesis observed in diabetes [1].In vivo:References:[1]. Laverdy OG, et al. Effects of glycemic control upon serum lipids and lipid transfers to HDL in patients with type 2 diabetes mellitus: novel findings in unesterified cholesterol status. Experimental and Clinical Endocrinology & Diabetes, 2015, 123(4):232–239[2]. Sandy Huey–Jen Hsu, et al. Validation of the Estimation of Low–density Lipoprotein Cholesterol by the Modified Friedewald Equation in Ethnic Chinese Adults Living in Taiwan. Internal Medicine, 54: 2291–2297, 2015[3]. Fukui K, et al. Effect of Cholesterol Reduction on Receptor Signaling in Neurons. J Biol Chem. 2015 Sep 14.Product Name:Cholesterol Cat. No.:HY-N0322CAS No.:57-88-5Molecular Formula:C 27H 46O Molecular Weight:386.65Target:Estrogen Receptor/ERR Pathway:Others Solubility:DMSO: 0.79 mg/mL (Need warming)Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@ Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

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Certificate of Analysis

PHYSICAL AND CHEMICAL PROPERTIES 

Molecular Formula:C19H16O4

Molecular Weight:308.33

Storage:Powder-20°C3 years4°C2 yearsIn solvent-80°C6 months-20°C1 monthChemical Structure:

ANALYTICAL DATA 

Appearance:White to off-white (Solid)1 H NMR Spectrum:Consistent with structureLCMS:Consistent with structurePurity (LCMS):99.45%Conclusion:The product has been tested and complies with the given specifications.

Product Name:WarfarinCat. No.:HY-B0687CAS No.:81-81-2Batch No.:13554Chemical Name:2H-1-Benzopyran-2-one, 4-hydroxy-3-(3-oxo-1-phenylbutyl)-

Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@MedChemExpress.comAddress: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA

Product Name:Aliskiren CAS No.:173334-57-1Cat. No.:HY-12176Product Data SheetMWt:551.76Formula:C30H53N3O6Purity :>98%Solubility:DMSOMechanisms:Biological Activity:Aliskiren(CGP 60536)is a direct renin inhibitor with IC50of 15nM Pathways:Metabolism/Protease; Target:ReninAliskiren(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM.IC50 value: 1.5 nM [1]Target: renin in vitro: Aliskiren hemifumarate appears to bind to both the hydrophobic S1/S3-binding pocket and to a large, distinct subpocket that extends from the S3-binding site towards the hydrophobic core of renin. Oral bioavailability of Aliskiren hemifumarate is 2.4% in rats, 16% in marmosets and about2.5% in humans [2].in vivo: Aliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets[3].Once-daily oral treatment with Aliskiren hemifumarate References:[1]. Yuji Nakamura, et al. Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. ACSMed. Chem. Lett., 2012, 3 (9), pp 754–758[2]. Buczko W, et al. Pharmacokinetics and pharmacodynamics of aliskiren, an oral direct renin p p []ylowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension[4]....[],p y ,inhibitor. Pharmacol Rep. 2008 Sep-Oct;60(5):623-31.[3]. Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renininhibitor.Biochem Biophys Res Commun, 2003, 308(4), 698-705.[4]. Gradman AH, et al.Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation, 2005,111(8), 1012-1018.Caution: Not fully tested. For research purposes onlyMedchemexpress LLC18 W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S AE m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m。

Product Name:Ezetimibe CAS No.:163222-33-1Cat. No.:HY-17376Product Data SheetMWt:409.43Formula:C24H21F2NO3Purity :>98%Solubility:DMSOMechanisms:Biological Activity:Ezetimibe a cholesterol absorption inhibitor reduces levels of low density lipoprotein (LDL) Pathways:Others; Target:Others Ezetimibe, a cholesterol-absorption inhibitor, reduces levels of low-density lipoprotein (LDL)cholesterol when added to statin treatment.IC50 value:Target: cholesterol-absorption Ezetimibe is a lipid-lowering drug that inhibits the intestinal absorption of dietary and biliary cholesterol by blocking passage across the intestinal wall. In patients with familialhypercholesterolemia, combined therapy with ezetimibe and simvastatin did not result in a significant difference in changes in intima-media thickness, as compared with simvastatin alone, despite decreases in levels of LDL cholesterol and C-reactive protein. ( number,References:[1]. Xiaobo Lin, Susan B. Racette, Michael Lefevre, et al. Combined Effects of Ezetimibe and Phytosterols on Cholesterol Metabolism: A Randomized, Controlled Feeding Study in Humans.Circulation. 2011; 124(5): 596-601.p (gNCT00552097.) Ezetimibe offers a new therapeutic option for patients receiving statins who require further reduction in LDL cholesterol....;()[2]. Anne B. Rosseb?, Terje R. Pedersen, Kurt Boman, et al. Intensive Lipid Lowering withSimvastatin and Ezetimibe in Aortic Stenosis. N Engl J Med 2008; 359:1343-1356.[3]. John J.P. Kastelein, Fatima Akdim, Erik S.G. Stroes, et al. Simvastatin with or without Ezetimibein Familial Hypercholesterolemia. N Engl J Med ,2008; 358:1431-1443.[4]. Christie M. Ballantyne, John Houri, Alberto Notarbartolo, et al. Effect of EzetimibeCoadministered With Atorvastatin in 628 Patients With Primary Hypercholesterolemia. ClinicalInvestigation and Reports Circulation. 2003; 107: 2409-2415.[5]. Claude Gagne?, Harold E. Bays, Stuart R. Weiss, et al. E...Caution: Not fully tested. For research purposes onlyMedchemexpress LLC18 W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S AE m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m。