118 products were found matching "K17689"!

Alprazolam is a benzodiazepine with anxiolytic and sedative actions. 4-Hydroxyalprazolam is a major metabolite of alprazolam, produced by the actions of cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5. It may be detected in serum or, in a glucuronidated form, in urine. Alternatively, 4-hydroxyalprazolam can be...

N-Acetyl-4-benzoquinone imine (NAPQI) is a cytochrome P450 3A4 and 2E1 metabolite of acetaminophen that can be toxic to the liver when acetaminophen is consumed in large doses. At therapeutic doses of acetaminophen, NAPQI is inactivated by conjugation with glutathione. However, following toxic doses of...

Voriconazole N-oxide is a major metabolite of the triazole antifungal voriconazole (Cay-15633). It is formed via oxidation of voriconazole by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C19.Formal Name:...

Naringin is a natural flavanone glycoside formed from naringenin and neohesperidose. It undergoes extensive metabolism in the liver, giving rise to naringenin and other bioactive metabolites that have anti-oxidant, anti-inflammatory, and anti-apoptotic effects. Naringin is a weak inhibitor of CYP3A4, providing 14%...

SB 202190 (Cay-10010399) and SB 203580 (Cay-13067) are potent, selective inhibitors of the MAP kinases p38alpha and p38beta. SB 202474 is a structural analog of SB 202190 and SB 203580 that is used as a negative control in studies of p38 inhibition.Formal Name:...

Resorufin benzyl ether is a fluorometric probe that acts as a substrate for cytochrome P450 (CYP)3A4. It is typically used near its apparent Km value of 30 µM to screen the inhibition/activation potential of test compounds, to predict potential drug-drug interactions, or to monitor other CYP450 activities. Upon...

Monocrotaline is a natural 11-membered macrocyclic pyrrolizidine alkaloid used in an animal model of pulmonary hypertension. It is metabolized by cytochrome P450 3A4 in the liver to monocrotaline pyrrole. Administration of monocrotaline or its metabolite monocrotaline pyrrole to rats causes progressive lung injury...

Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources). It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms. Azamulin potently blocks the...

11beta-hydroxy Testosterone is a metabolite of testosterone. It is formed from testosterone primarily by the cytochrome P450 (CYP) isoform CYP3A4.Formal Name: 11beta,17beta-dihydroxy-androst-4-en-3-one. CAS Number: 1816-85-9. Synonyms: NSC 12168. Molecular Formula: C19H28O3. Formula Weight: 304.4. Purity: >95%....

PF-04981517 is a potent, time-dependent inhibitor of the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 30 nM). It is less effective against CYP3A5 and CYP3A7 (IC50s = 17 and 70 µM, respectively). PF-04981517 will be useful for understanding the relative roles of CYP3A4 and CYP3A5 in drug metabolism.Formal Name:...

5-hydroxy Diclofenac is an active metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor diclofenac (Cay-70680, Cay-22983). It is formed by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C9, CYP2C19, and CYP1A2. 5-hydroxy Diclofenac is cytotoxic to HL-60 leukemia cells (IC50 = 661 µM). It...

Stiripentol is a third-generation antiepileptic compound. It is a positive allosteric modulator of GABAA receptors, potentiating GABA-mediated activation to a greater extent in receptors expressing alpha3 subunits and to a lower extent in those containing beta1 or epsilon subunits. It also inhibits GABA reuptake in...