Geneknown™ Hepatocytes

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Sekisui XenoTech's Geneknown™ hepatocytes are characterized for pharmacologically relevant polymorphisms affecting the ADMET properties of xenobiotics.

Genetically determined transport and metabolism polymorphisms have been recognized by the FDA as having potential safety and efficacy implications. This is particularly important for poor metabolizers in cases of drugs metabolized predominantly by polymorphically expressed enzymes. Geneknown hepatocytes™ are pooled to study the effects of specific genetic variants on drug metabolism and transport to identify risks of adverse drug interactions present only in genetically-defined subpopulations of patients.

The following genes were evaluated for the presence of significant alleles and SNPs (single nucleotide polymorphisms):

  • CYP1A1, 1A2, 2A6, 2B6, 2D6, 2C8, 2C9, 2C19, 2E1, 3A4, 3A5
  • MDR1 (ABCB1), MRP2 (ABCC2), BCRP (ABCG2), PEPT2 (SLC15A2), OCT1 (SLC22A1), OCT2 (SLC22A2), OAT1 (SLC22A6), OATP1B1 (SLCO1B1), OATP1B3 (SLCO1B3), OATP2B1 (SLCO2B1)
  • DPYD (dihydropyrimidine dehydrogenase), GSTP1 (glutathione S-transferase pi 1), NAT1 (N-acetyltransferase 1), NAT2 (N-acetyltransferase 2), TPMT (thiopurine S-methyltransferase), UGT1A1 (UDP glucuonosyltransferase 1 family polypeptide A1), UGT2B15 (UDP glucuronosyltransferase 2 family polypeptide B15), UGT2B7 (UDP glucuronosyltransferase 2 family polypeptide B7), VKORC1 (vitamin K epoxide reductase complex subunit 1)
 

A full list of the alleles and SNP IDs comprising the characterization of Geneknown™ human hepatocytes can be found here.

Geneknown™ cryopreserved human hepatocytes are offered as pools of cryopreserved cells from multiple donors assembled to study the effects of individual genetic variants. Geneknown™ hepatocytes are cryopreserved using the same proprietary single-freeze method that we use with our CryostaX® product.

Highlights of Geneknown™ hepatocytes:

  • CYP2C19*2/*2 no activity homozygotes and CYP2C19*1/*1 wild-type controls
  • Complex genetics of CYP2D gene cluster are characterized with 25 individual SNP assays, as well as, CYP2D6 and CYP2D7 gene copy number variation assays, allowing identification of ultra-rapid, extensive and poor metabolizers
  • CYP3A5*1/*1 high-activity homozygotes, CYP3A5*1/*3 intermediate activity heterozygotes and CYP3A5*3/*3 no-activity control cells
  • UGT1A1 low-activity donors carrying two alleles of reduced activity and wild-type UGT1A1*1/*1 control donors
  • OATP1B1*5/*5 homozygotes and wild-type OATP1B1*1/*1 control cells

Related Products: Buy cell and tissue based products
Product Description
HPCH.2C19.HA Genotyped CYP2C19 - High Activity (*1/*1) - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.2C19.MA Genotyped CYP2C19 - Moderate Activity (*1/*2) - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.2C19.NA Genotyped CYP2C19 - No Activity (*2/*2) - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.2C8.HA Genotyped CYP2C8 - High Activity (*1/*1) - Cryopreserved Pooled Human Hepatocytes- Suspension
HPCH.2C8.MA Genotyped CYP2C8 - Medium Activity -- Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.2C9.HA Genotyped CYP2C9 - High Activity (*1/*1 ) - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.2C9.MA Genotyped CYP2C9 - Moderate Activity - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.2D6.HA Genotyped CYP2D6 -High Activity - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.2D6.MA Genotyped CYP2D6 - Moderate Activity - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.2D6.NA Genotyped CYP2D6 - No Activity - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.3A5.HA Genotyped CYP3A5 - High Activity - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.3A5.MA Genotyped CYP3A5 - Moderate Activity (*1/*3) - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.3A5.NA Genotyped CYP3A5 - No Activity (*3/*3) - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.OATP1B1.HA Genotyped OATP1B1 - High Activity - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.OATP1B1.MA Genotyped OATP1B1 - Moderate Activity - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.UGT1A1.HA Genotyped UGT1A1 - High Activity (*1/*1) - Cryopreserved Pooled Human Hepatocytes - Suspension
HPCH.UGT1A1.MA Genotyped UGT1A1 - Moderate Activity - Cryopreserved Pooled Human Hepatocytes - Suspension
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