Geneknown™ hepatocytes for suspension are genotyped and characterized for pharmacologically relevant polymorphisms affecting the enzymatic activity or function of proteins known to be involved in the pharmacokinetic and toxicological properties of xenobiotics.
GeneknownTM Genotyped Human Hepatocytes for Suspension
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Geneknown™ suspension cryopreserved human hepatocytes, hepatic cells containing many drug-metabolizing enzymes, are offered as pools of cryopreserved cells from multiple donors assembled to study the effects of individual genetic variants. 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 make it possible for researchers to investigate 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)
Highlights of Geneknown™ hepatocytes
- Cryopreserved using the same proprietary single-freeze method that we use with our CryostaX® products
- 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
Match your test systems with the right media
Our formulas are optimized to give you the best results from your hepatocytes in suspension. Read our media guide to maximize performance and output of your hepatocyte assays
