Ultrapool human liver microsomes

Manufactured by Corning

Sourced in United States

UltraPool human liver microsomes are a laboratory product that consists of subcellular fractions derived from human liver tissue. They are used as a tool for in vitro studies related to drug metabolism and toxicology research.

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Human liver microsomes (9 citations) Liver microsomes (2 citations)

3 protocols using ultrapool human liver microsomes

Characterization of Human Liver Microsomes

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UltraPool human liver microsomes (150-donor pooled, mixed gender), lot number 38291 (452117), and single-donor human liver microsomes from lot number HH581, male (452138), were purchased from Corning Life Sciences (Tewksbury, MA). For donor HH581, the liver microsomal P450 1A2 activity, as measured by phenacetin O-deethylation, was 2100 pmol/mg protein/min (reported by Corning Life Sciences). Human liver microsomes from individual donors genotyped for CYP3A5 were purchased from Corning Life Sciences and Xenotech (Kansas City, KS). The individual donor lot numbers, sex, and CYP3A5 genotypes reported by each company were as follows: (i) human liver microsomes from Corning Life Sciences, CYP3A5*1/*1 donors HH860 (female), HH867 (male), HH785 (male); CYP3A5*1/*3 donors HH757 (male), HH868 (male); CYP3A5*3/*3 donors HH189 (female), HH507 (male); (ii) human liver microsomes from Xenotech, CYP3A5*1/*1 donor 710272 (female); CYP3A5*1/*3 donor 710232 (female); CYP3A5*3/*3 donors 710252 (male), 710253 (male), 710237 (male), as described previously.^{30 (link)} Donor information is provided in Table S1.

Burnham E.A., Abouda A.A., Bissada J.E., Nardone-White D.T., Beers J.L., Lee J., Vergne M.J, & Jackson K.D. (2022). Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation. Chemical research in toxicology, 35(5), 792-806.

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Comprehensive In Vitro ADME Toolkit

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Corning UltraPool human liver microsomes (HLM) 150 (20 mg/mL), human intestinal microsomes (HIM) pool (10 mg/mL) as well as recombinant human CYP enzymes (with P450 oxidoreductase, OR) including CYP1A2+OR (0.5 nmol), CYP2B6+OR (0.5 nmol), CYP2C8+OR (1.0 nmol), CYP2C9*1+OR (1 nmol), CYP2C19+OR (0.5 nmol), CYP2D6*1+OR (0.5 nmol), CYP2E1+OR + cytochrome b₅ (1 nmol), CYP3A4+OR + cytochrome b₅ (0.5 nmol), MAO-A (5 mg/mL), MAO-B (5 mg/mL), and UGT1A10 (5 mg/mL) were purchased from Corning Life Sciences B.V (Amsterdam, Netherlands). All microsomes and recombinant enzyme solutions were aliquoted and stored at −80 °C until further use. Co-factors including NADPH regenerating system solution A (25 mM NADP+, 66 mM glucose-6-phosphate, and 66 mM MgCl₂ in water), NADPH regenerating system solution B (40 U/mL glucose-6-phosphate dehydrogenase in 5 mM sodium citrate), UGT reaction mix solution A (25 mM uridine 5′-diphospho-glucuronic acid in water), and UGT reaction mix solution B (250 mM Tris-HCl, 40 mM MgCl₂, and 0.125 mg/mL alamethicin in water) were also obtained from Corning Life Sciences B.V.

Thomann J., Kolaczynska K.E., Stoeckmann O.V., Rudin D., Vizeli P., Hoener M.C., Pryce C.R., Vollenweider F.X., Liechti M.E, & Duthaler U. (2024). In vitro and in vivo metabolism of psilocybin’s active metabolite psilocin. Frontiers in Pharmacology, 15, 1391689.

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Characterization of AM-2201 Metabolism

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AM-2201 was purchased from Cayman Chemical Company (Ann Arbor, MI, USA). Acetaminophen, alamethicin, chenodeoxycholic acid, coumarin, diclofenac, 7-hydroxycoumarin, midazolam, mycophenolic acid, N-acetylserotonin, naloxone, naloxone 3-β-d-glucuronide, NADPH, phenacetin, trifluoperazine, Trizma^® base, and uridine 5′-diphospho-glucuronic acid (UDPGA) were purchased from Sigma-Aldrich (St. Louis, MO, USA). Ultrapool human liver microsomes (150 donors), ¹³C₂,¹⁵N-Acetaminophen, bufuralol, N-desethylamodiaquine, 1′-hydroxybufuralol, 4-hydroxy-diclofenac, 4-hydroxymephenytoin, d₃-4-hydroxymephenytoin, 1′-hydroxymidazolam, d₉-1-hydroxybufuralol, and [S]-mephenytoin were obtained from Corning Life Sciences (Woburn, MA, USA). SN-38 was obtained from Santa Cruz Biotechnology (Dallas, TX, USA). N-Acetylserotonin β-d-glucuronide, chenodeoxycholic acid-24-acyl-β-glucuronide, mycophenolic acid β-d-glucuronide, and SN-38 glucuronide were obtained from Toronto Research Chemicals (Toronto, ON, Canada). Acetonitrile and methanol (high performance liquid chromatography (HPLC) grade) were obtained from Fisher Scientific (Fair Lawn, NJ, USA). All other chemicals were of the highest quality available.

Kim J.H., Kwon S.S., Kong T.Y., Cheong J.C., Kim H.S., In M.K, & Lee H.S. (2017). AM-2201 Inhibits Multiple Cytochrome P450 and Uridine 5′-Diphospho-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes. Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry, 22(3), 443.

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