CYP2C9 Genotyped Microsomes

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XenoTech's genetically-defined products include human liver microsomes prepared from individual donors characterized for various CYP2C9 alleles corresponding to high activity, moderate activity and no activity.
 
CYP2C9 is the second most abundant CYP, following CYP3A4, in the human liver. It plays a dominant role in the metabolism of ~10% of all therapeutic drugs, including a wide variety of analgesics, anti-infectives, NSAIDs, oral hypoglycemics, anticoagulants, diuretics and antiepileptics. 
 
The two most common variant alleles are CYP2C9*2 and CYP2C9*3. These variants are due to SNPs (single-nucleotide polymorphisms) 430C>T and 1075A>C, respectively. CYP2C9 shows high inter-ethnic and intra-ethnic variability, with CYP2C9*2 and *3 frequency nearly 20% in some Caucasian populations and undetectable in some African American and Asian populations. The intrinsic clearance of drugs metabolized by CYP2C9*1 is usually greater than that of CYP2C9*2 or *3, with CYP2C9*2 usually having a greater rate than *3. CYP2C9*5 also shows decreased activity compared to the wild type and CYP2C9*6 shows no activity. Detailed descriptions of the nucleotide changes characterizing individual alleles and their effects on protein expression and the CYP2C9 phenotype can be found at www.cypalleles.ki.se.
 
Most common variants: CYP2C9*2 and CYP2C9*3. Low frequency alleles CYP2C9*5 and CYP2C9*6, identified in African Americans, are characterized by decrease and no activity, respectively.

CYP2C9 Allele Frequency
 
Allele African
American
Asian Caucasian Hispanic
CYP2C9*1 0.94 - 0.995 0.88 - 0.989 0.695 - 0.940 0.849 - 0.922
CYP2C9*2 0.0 - 0.04 0.0 - 0.04 0.08 - 0.191 0.048 - 0.12
CYP2C9*3 0.0 - 0.023 0.011 - 0.13 0.033 - 0.17 0.0 - 0.066
CYP2C9*5 0.017 - 0.13 ND ND ND
CYP2C9*6 0.006 ND ND ND
ND = Not detected
Adapted from Scordo, et.al, 2001, Yoon, et. al, 2001, Dickman, et. al, 2001, Blaisdell, et. al, 2004, Kirchheiner, et. al, 2004, DeLozier, et. al, 2005, Garcia-Martin, et. al, 2006 and Rosemary and Adithan, 2007.
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Product Description Volume
H2C9.HA Individual human liver microsomes, Genotyped for CYP2C9, high activity, 20mg/mL 0.5mL
H2C9.MA Individual human liver microsomes, Genotyped for CYP2C9, moderate activity, 20mg/mL 0.5mL
*All genotyped human liver microsomes are supplied at a protein concentration of 20 mg/mL in 250 mM sucrose
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