The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4. In a Article£¬once mentioned of 125995-03-1, COA of Formula: C33H33FN2O4
The metabolism of clopidogrel is catalyzed by human cytochrome P450 3A and is inhibited by atorvastatin
The prodrug clopidogrel (Plavix) is activated by cytochrome P450 (P450) to a metabolite that inhibits ADP-induced platelet aggregation. Clopidogrel is frequently administered to patients in conjunction with the CYP3A4 substrate atorvastatin (Lipitor). Since clinical studies indicate that atorvastatin inhibits the antiplatelet activity of clopidogrel, we investigated whether CYP3A4 metabolized clopidogrel in vitro. Microsomes prepared from dexamethasone-pretreated rats metabolized clopidogrel at a rate of 3.8 nmol min-1 nmol of P450-1, which is 65 and 1270% faster than the rate of metabolism by microsomes from control and beta-napthoflavonetreated rats, respectively. To identify the human P450s responsible for clopidogrel oxidation, genetically engineered microsomes containing a single human P450 isozyme were tested for their ability to oxidize clopidogrel. CYP3A4 and 3A5 metabolized clopidogrel at a significantly higher rate than eight other P450 isozymes, suggesting that CYP3A4 and 3A5 are primarily responsible for in vivo clopidogrel metabolism. Clopidogrel interacts with human CYP3A4 with a spectral dissociation constant (Ks), Km, and Vmax of 12 muM, 14 ¡À muM and 6.7 ¡À 1 nmol min-1 nmol P450-1, respectively. Atorvastatin lactone, the physiologically relevant substrate, inhibits clopidogrel with a KI of 6 muM. When clopidogrel and atorvastatin are present at equimolar concentrations, clopidogrel metabolism is inhibited by greater than 90%. Since CYP3A4 and 3A5 metabolize clopidogrel faster than other human P450 isozymes and are the most abundant P450s in human liver, they are predicted to be predominantly responsible for the activation of clopidogrel in vivo.
Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.COA of Formula: C33H33FN2O4, you can also check out more blogs about125995-03-1
Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics