Atorvastatin lactone

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Cat No: 20951

Biochemicals - Small Molecule Inhibitors

Atorvastatin lactone is an active metabolite of the HMG-CoA reductase inhibitor atorvastatin.{62437,32970} It is formed from atorvastatin by the UDP-glucuronosyltransferase (UGT) isoforms UGT1A3 and UGT1A1 in insect cell-derived supersomes expressing ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1H-pyrrole-3-carboxamide

Correlated keywords:

142062-65-5 prodrug metabolite HMG-CoA reductase uridine 5’-diphospho-glucuronosyltransferases P-glycoprotein pro-drug d-lactone ?-lactone glucuronosyl-transferase

Product Overview:
Atorvastatin lactone is an active metabolite of the HMG-CoA reductase inhibitor atorvastatin.{62437,32970} It is formed from atorvastatin by the UDP-glucuronosyltransferase (UGT) isoforms UGT1A3 and UGT1A1 in insect cell-derived supersomes expressing the human enzymes, and hydrolyzes to form atorvastatin in human serum at room temperature.{32970,32969} Atorvastatin lactone inhibits HMG-CoA reductase (IC50 = 0.007 µM for the rat liver enzyme).{62437} It also inhibits the cytochrome P450 (CYP) isoforms CYP2C9.1 and CYP2C9.3 (IC50s = 16.8 and 5.62 µM, respectively), as well as P-glycoprotein (P-gp; IC50 = 3.1-5.2 µM).{59946,32967}

Size	1 mg
Shipping	dry ice
CAS Number	125995-03-1
Molecular Formula	C₃₃H₃₃FN₂O₄
SMILES	O=C(C1=C(C(C)C)N(CC[C@H](C[C@@H](O)C2)OC2=O)C(C3=CC=C(F)C=C3)=C1C4=CC=CC=C4)NC5=CC=CC=C5
Molecular Weight	540,6
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2922.19
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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