In vitro metabolism of rivaroxaban, an oral, direct factor Xa inhibitor, in liver microsomes and hepatocytes of rats, dogs, and humans.

In vitro metabolism of rivaroxaban, an oral, direct factor Xa inhibitor, in liver microsomes and hepatocytes of rats, dogs, and humans. post thumbnail image

The in vitro metabolism of rivaroxaban, a novel, oral, direct issue Xa inhibitor for the prevention and remedy of thromboembolic issues, was investigated in a number of species, together with people. The target of this research was to elucidate metabolite constructions and establish the metabolic pathways to offer assist for in vivo security and medical research. [(14)C]Rivaroxaban was incubated with liver microsomes and hepatocytes of rats, canine, and people. The samples had been analyzed by high-performance liquid chromatography-(14)C-tandem mass spectroscopy, to generate metabolite profiles and suggest or affirm the constructions of the metabolites shaped. In vitro metabolite profiles confirmed no main variations between species.

The principle oxidative metabolic pathways recognized for all species had been hydroxylation on the morpholinone moiety (M-2, M-3, and M-8) and to a lesser extent on the oxazolidinone moiety (M-9). M-2 was the primary metabolite in all microsomal incubations. M-1, a morpholinone ring-opened product shaped by additional oxidation of M-2, was the primary metabolite in all hepatocyte incubations. Different pathways had been amide hydrolysis on the morpholinone ring (M-7) and the chlorothiophene amide moiety (M-13 and M-15). In hepatocytes, M-13 was readily conjugated with glycine, resulting in M-4. The metabolic destiny of unlabeled M-15 was investigated individually.

Incubations with human liver microsomes and hepatocytes confirmed that M-15 was first oxidized to the aldehyde intermediate M-16 and subsequently diminished to M-17 (alcohol) or oxidized to M-18 (carboxylic acid). No metabolism on the chlorothiophene moiety itself was discovered. Total, rivaroxaban confirmed no species variations in metabolism, with completely different unbiased metabolic pathways and no formation of reactive metabolites.

In vivo clearance predictions from in vitro assays require scaling elements to narrate the concentrations of hepatocytes or microsomal protein to the intact liver. 2. The goals had been to measure the variability in scaling elements for Wistar rat and beagle canine for which the literature is especially scarce and decide any intercourse variations. 3. Scaling elements had been decided by evaluating the cytochrome P450 (P450) content material in hepatocytes or microsomes in opposition to the P450 content material of recent liver homogenate. Using recent homogenate is really helpful as freezing can improve contamination and have an effect on the P450 assay.

Comparability of genistein metabolism in rats and people utilizing liver microsomes and hepatocytes.

Species variations and metabolism are probably the most essential elements in contemplating the results of genistein. The goal of this research was to have a greater information of the metabolic destiny of genistein in people as in contrast with rats. For this goal, radiolabeled genistein was incubated with human and rat liver microsomes and with cryopreserved hepatocytes from each species. Incubations had been carried out utilizing a variety of genistein concentrations to research the kinetics of formation of the metabolites. Metabolite profiling was obtained utilizing an HPLC system linked to a radioactivity detector.

In vitro metabolism of rivaroxaban, an oral, direct factor Xa inhibitor, in liver microsomes and hepatocytes of rats, dogs, and humans.

Identification of the metabolites was primarily based on their retention occasions as in contrast with these of genuine requirements and on LC-MS (ESI-MS/MS) or NMR analyses. In each species, liver microsomes produced the identical three hydroxylated metabolites (8-OH, 6-OH and three’-OH-genistein) whereas cryopreserved hepatocytes produced the identical glucurono- and sulfo-conjugates (genistein 4′-O-sulfate 7-O-glucuronide, genistein 7-O-glucuronide, genistein 4′-O-glucuronide, genistein 7-O-sulfate and genistein 4′-O-sulfate). The speed of metabolism assorted with species. 3′-Hydroxygenistein was the predominant metabolite produced by rat liver microsomes, whereas in people 3′-hydroxy and 8-hydroxygenistein had been produced in the identical vary.

Metabolism of prazosin in rat, canine, and human liver microsomes and cryopreserved rat and human hepatocytes and characterization of metabolites by liquid chromatography/tandem mass spectrometry.

Prazosin (2-[4-(2-furanoyl)-piperazin-1-yl]-4-amino-6,7-dimethoxyquinazoline) is an antihypertensive agent that was launched to the market in 1976. It has since established a wonderful security document. Nonetheless, in vitro metabolism of prazosin has not been investigated. This research describes the in vitro biotransformation of prazosin in liver microsomes from rats, canine, and people, in addition to rat and human cryopreserved hepatocytes and characterization of metabolites utilizing liquid chromatography/tandem mass spectrometry. The main in vivo biotransformation pathways reported beforehand in rats and canine embody demethylation, amide hydrolysis, and O-glucuronidation.

These metabolic pathways had been additionally confirmed in our research. As well as, a number of new metabolites had been characterised, together with a secure carbinolamine, an iminium species, and an enamine-all shaped by way of oxidation of the piperazine ring. Two ring-opened metabolites generated following oxidative cleavage of the furan ring had been additionally recognized. Utilizing semicarbazide hydrochloride as a trapping agent, an intermediate arising from opening of the furan ring was captured as a pyridazine product. Within the presence of glutathione, three glutathione conjugates had been detected in microsomal incubations, though they weren’t detected in cryopreserved hepatocytes.

Total Protein - Human Adult Normal Tissue: Seminal Vesicle

P1234214 1 mg
EUR 513

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IRHUSMF1ML each
EUR 247
Description: Pooled Human Seminal Fluid

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IRHUSMF5ML each
EUR 690
Description: Pooled Human Seminal Fluid

Mouse Seminal vesicle secretory protein 6, Svs6 ELISA KIT

ELI-41757m 96 Tests
EUR 1038

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ELI-23600m 96 Tests
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ELI-19037m 96 Tests
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Seminal Plasma, Human Protein

abx069938-10ml 10 ml
EUR 1111.2

Rat Secreted seminal- vesicle Ly- 6 protein 1, Sslp1 ELISA KIT

ELI-42469r 96 Tests
EUR 1063.2

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ELI-41041m 96 Tests
EUR 1038

Bovine Secreted seminal- vesicle Ly- 6 protein 1, SSLP1 ELISA KI

ELI-18704b 96 Tests
EUR 1113.6

Lactoferrin (Seminal Plasma) Protein

20-abx262658
  • EUR 393.60
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  • EUR 276.00
  • 10 ug
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  • 2 µg

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EUR 1113.6

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Single Donor Human Seminal Fluid

IRHUSSMF1ML each
EUR 247
Description: Single Donor Human Seminal Fluid

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IRHUSSMF5ML each
EUR 689
Description: Single Donor Human Seminal Fluid

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Seminal Plasma Inhibin (67-94) (human)

H-1602.0500 0.5mg
EUR 400.8
Description: Sum Formula: C150H240N36O43S2; CAS# [96182-95-5]

Seminal Plasma Inhibin (67-94) (human)

H-1602.1000 1.0mg
EUR 691.2
Description: Sum Formula: C150H240N36O43S2; CAS# [96182-95-5]

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ELI-40880b 96 Tests
EUR 1113.6

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Svs3b (Myc-DDK-tagged ORF) - Rat seminal vesicle secretory protein 3B (Svs3b), (10 ug)

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Rat seminal plasma protein homolog 1 ELISA kit

E02B0856-192T 192 tests
EUR 1524
Description: A sandwich ELISA for quantitative measurement of Rat seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Rat seminal plasma protein homolog 1 ELISA kit

E02B0856-48 1 plate of 48 wells
EUR 624
Description: A sandwich ELISA for quantitative measurement of Rat seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Rat seminal plasma protein homolog 1 ELISA kit

E02B0856-96 1 plate of 96 wells
EUR 822
Description: A sandwich ELISA for quantitative measurement of Rat seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Dog seminal plasma protein homolog 1 ELISA kit

E08B0856-192T 192 tests
EUR 1524
Description: A sandwich ELISA for quantitative measurement of Canine seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Dog seminal plasma protein homolog 1 ELISA kit

E08B0856-48 1 plate of 48 wells
EUR 624
Description: A sandwich ELISA for quantitative measurement of Canine seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Dog seminal plasma protein homolog 1 ELISA kit

E08B0856-96 1 plate of 96 wells
EUR 822
Description: A sandwich ELISA for quantitative measurement of Canine seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Pig seminal plasma protein homolog 1 ELISA kit

E07B0856-192T 192 tests
EUR 1524
Description: A sandwich ELISA for quantitative measurement of Porcine seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Pig seminal plasma protein homolog 1 ELISA kit

E07B0856-48 1 plate of 48 wells
EUR 624
Description: A sandwich ELISA for quantitative measurement of Porcine seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Pig seminal plasma protein homolog 1 ELISA kit

E07B0856-96 1 plate of 96 wells
EUR 822
Description: A sandwich ELISA for quantitative measurement of Porcine seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Rat seminal plasma protein homolog 1 ELISA kit

E01A10661 96T
EUR 700
Description: ELISA

Lenti ORF clone of Svs3a (Myc-DDK-tagged ORF) - Rat seminal vesicle secretion 3 (Svs3), (10 ug)

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Goat seminal plasma protein homolog 1 ELISA kit

E06B0856-192T 192 tests
EUR 1524
Description: A sandwich ELISA for quantitative measurement of Goat seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Goat seminal plasma protein homolog 1 ELISA kit

E06B0856-48 1 plate of 48 wells
EUR 624
Description: A sandwich ELISA for quantitative measurement of Goat seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Goat seminal plasma protein homolog 1 ELISA kit

E06B0856-96 1 plate of 96 wells
EUR 822
Description: A sandwich ELISA for quantitative measurement of Goat seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Goat seminal plasma protein homolog 1 ELISA kit

E01A45573 96T
EUR 700
Description: ELISA

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MR218264L3 10 µg Ask for price

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LTF S.Plasma Lactoferrin Human (Seminal Plasma) protein

PROTP02788-2 Regular: 10ug
EUR 380.4
Description: The Human Lactoferrin produced from pooled Human seminal plasma has a molecular mass of 76.165kDa (calculated without glycosylation) containing 691 amino acid residues.

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Human seminal plasma protein homolog 1 ELISA kit

E01B0856-192T 192 tests
EUR 1524
Description: A sandwich ELISA for quantitative measurement of Human seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Human seminal plasma protein homolog 1 ELISA kit

E01B0856-48 1 plate of 48 wells
EUR 624
Description: A sandwich ELISA for quantitative measurement of Human seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Human seminal plasma protein homolog 1 ELISA kit

E01B0856-96 1 plate of 96 wells
EUR 822
Description: A sandwich ELISA for quantitative measurement of Human seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Mouse seminal plasma protein homolog 1 ELISA kit

E03B0856-192T 192 tests
EUR 1524
Description: A sandwich ELISA for quantitative measurement of Mouse seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Mouse seminal plasma protein homolog 1 ELISA kit

E03B0856-48 1 plate of 48 wells
EUR 624
Description: A sandwich ELISA for quantitative measurement of Mouse seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

Mouse seminal plasma protein homolog 1 ELISA kit

E03B0856-96 1 plate of 96 wells
EUR 822
Description: A sandwich ELISA for quantitative measurement of Mouse seminal plasma protein homolog 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. This is a high quality ELISA kit developped for optimal performance with samples from the particular species.

These information assist ring opening of the furan by way of a reactive gamma-keto-alpha,beta-unsaturated aldehyde intermediate. Within the presence of UDP-glucuronic acid, prazosin underwent conjugation to type an N-glucuronide not reported beforehand. Our in vitro investigations have revealed further metabolic transformations of prazosin and have proven the potential of prazosin to endure bioactivation by means of metabolism of the furan ring to a reactive intermediate.

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