minor metabolite

Dasatinib N-oxide is a minor metabolite of Dasatinib.Dasatinib is an orally potent inhibitor of Src Bcr-Abl.

3-Hydroxyhippuric acid is an acyl glycine, typically a minor metabolite of fatty acids [acyl glycines].

Suberylglycine is an acyl glycine that is a normally minor metabolite of fatty acid.

1,3,7-Trimethyluric acid, a purine alkaloid, occurs as a minor metabolite of caffeine in humans. It functions as an antioxidant with the ability to scavenge hydroxyl radicals and offers protective benefits against lipid peroxidation in erythrocyte membranes.

3,4-Dihydroxyamphetamine (α-Methyldopamine) (hydrochloride) is a minor metabolite of 3,4-Methylenedioxymethamphetamine (MDMA) and exhibits cytotoxicity in rat hepatocytes. Additionally, 3,4-Dihydroxyamphetamine (hydrochloride) is applicable in hypertension research.

17-Oxosparteine is a minor urinary metabolite of sparteine in man.

Adriamycin Aglycone, also known as Doxorubicinone, is an oncolytic agent. It is a metabolite of Doxorubicin which binds to the DNA minor-groove.

Rugulin is a minor metabolite from Penicillium rugulosum and a naturally occurring bisanthraquinone.

Valinotricin is a minor fungal metabolite.

(-)-Sitagliptin carbamoyl glucuronide is a minor phase II metabolite of the dipeptidyl peptidase 4 (DPP-4) inhibitor (-)-sitagliptin . (-)-Sitagliptin carbamoyl glucuronide is formed by N-carbamoyl glucuronidation and has been found in rat and dog plasma following administration of (-)-sitagliptin.

Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. (±)16-HETE is the racemic version of a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation. The biological activity of 16-HETE is stereospecific. 16(R)-HETE dose-dependently stimulates vasodilation of the rabbit kidney, however 16(S)-HETE does not affect perfusion pressure. At a concentration of 2 μM the (S)-enantiomer of 16-HETE inhibits proximal tubule ATPase activity by as much as 60%, whereas the (R)-isomer has negligible effects on ATPase activity.

Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. 16(S)-HETE inhibits proximal tubule ATPase activity by as much as 60% at a concentration of 2 µM.[1]

Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. 16(S)-HETE inhibits proximal tubule ATPase activity by as much as 60% at a concentration of 2 μM.

Oligomycin E is a minor metabolite of the oligomycin complex produced by several species of Streptomyces. It exhibits relatively weak antifungal activity compared to other oligomycins, yet is active against Gram-positive bacteria and demonstrates strong antitumor activity against HeLa cells (IC50 = 14 ng/ml).

Avanafil metabolite M16 is a major inactive metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil . Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M16 and avanafil metabolite M4 , as well as minor metabolites.

Avanafil metabolite M4 is a major active metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil . Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M4 and avanafil metabolite M16 , as well as minor metabolites. Avanafil metabolite M4 inhibits PDE5 with 18% of the potency of avanafil.

Celecoxib carboxylic acid acyl-β-D-glucuronide is a phase II metabolite of celecoxib . Celecoxib is an anti-inflammatory compound from the diaryl heterocycle class that selectively inhibits cyclooxygenase-2 (COX-2; IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively). Celecoxib carboxylic acid acyl-β-D-glucuronide is a minor metabolite, accounting for 2% of the administered dose in human urine and rat bile.

Carbazomycin D is a bacterial metabolite that has been found inStreptomycesand has diverse biological activities.1,2It is active against the fungiT. asteroidesandT. mentagrophytes(MIC = 100 μg ml for both) and the bacteriumM. tuberculosis(IC50= 25 μg ml). Carbazomycin D is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 21.3, 33.2, 12.9, and 34.3 μg ml, respectively).2 1.Naid, T., Kitahara, T., Kaneda, M., et al.Carbazomycins C, D, E and F, minor components of the carbazomycin complexJ. Antibiot. (Tokyo)40(2)157-164(1987) 2.Intaraudom, C., Rachtawee, P., Suvannakad, R., et al.Antimalarial and antituberculosis substances from Streptomyces sp. BCC26924Tetrahedron67(39)7593-7597(2011)

3-hydroxy Lignoceric acid is a hydroxylated form of the 24-carbon saturated lignoceric acid . 3-hydroxy Lignoceric acid is found in minor amounts in Methyloligella, a novel Gram-negative bacteria. 3-hydroxy Lignoceric acid, in the form of an acyl-CoA metabolite, is an intermediate in fatty acid chain elongation from docosanoic acid to lignoceric acid (C24:0).

Fenbendazole sulfone is a minor metabolite of the anthelmintic fenbendazole . Fenbendazole undergoes oxidation to form oxfendazole, which is further oxidized to form fenbendazole sulfone.

7(Z)-Tricosene is an insect pheromone and endogenous metabolite for mating and interspecific recognition.

Latanoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug. Oxidation of the C-15 hydroxyl group without isopropyl ester hydrolysis produces 15-keto latanoprost. 15-keto Latanoprost is a potential metabolite of latanoprost when administered to animals. 15-keto Latanoprost is also one of the common minor impurities found in commercial preparations of the bulk drug compound. Although much less potent that the parent compound latanoprost, 15-keto latanoprost still retains the ability to produce a small but measurable decrease (1 mm Hg) in the intraocular pressure of normal cynomolgus monkeys when administered at a dose of 1 μg/eye. 15-keto Latanoprost is also a miotic in the normal cat eye, causing an 8 mm reduction in pupillary diameter at 5 μg/eye. Again, this is not as potent as many other F-type PGs; for example, PGF2α will produce this degree of miosis at a dose of less than 1 μg/eye. Products of β-oxidation account for most of the metabolites of latanoprost recovered in plasma and urine. However, 15-keto latanoprost is a minor metabolite, and one which could be enhanced in situations where β-oxidation is reduced.

15-keto Latanoprost is a potential metabolite of latanoprost when administered to animals and is a common minor impurity in commercial preparations of the bulk drug compound. Although much less potent than latanoprost, 15-keto Latanoprost can still produce a small but measurable decrease (1 mm Hg) in intraocular pressure in normal cynomolgus monkeys at a dose of 1 μg eye. It also acts as a miotic in normal cats, causing an 8 mm Hg reduction in pupillary diameter at 5 μg eye, though it is not as potent as many other F-type prostaglandins, such as prostaglandin F2α, which achieves the same effect at less than 1 μg eye.

Bimatoprost is an F-series prostaglandin (PG) analog approved for use as an ocular hypotensive drug. Oxidation of the C-15 hydroxyl group and amide hydrolysis of Bimatoprost produces 15-keto-17-phenyl trinor PGF2α, a potential metabolite when administered to animals. 15-keto PG analogs can be minor impurities in commercial preparations of corresponding bulk drug compounds. Although much less potent than the parent compound, 15-keto PGs can still produce a small but measurable decrease (1 mm Hg) in intraocular pressure of normal cynomolgus monkeys at a dose of 1 μg eye. 15-keto Latanoprost (15-keto-17-phenyl-13,14-dihydro trinor PGF2α isopropyl ester) acts as a miotic in normal cat eyes, causing an 8 mm reduction in pupillary diameter at 5 μg eye. This is less potent compared to many other F-type PGs; for example, PGF2α induces similar miosis at less than 1 μg eye.