Human Liver Microsomes

View Products

PackagingCharacterization ProvidedProduct DetailsRelated Products

 

Human liver microsomes are used to evaluate metabolic stability and in vitro intrinsic clearance [Vmax/Km], to identify which cytochrome P450 (CYP) or UDP-glucuronosyltransferase (UGT) enzyme or enzymes are responsible for oxidizing or glucuronidating a drug candidate (a process known as reaction pheotyping or enzyme mapping), and to evaluate drug candidates as inhibitors of CYP and UGT enzymes.

Human liver microsomes con­tain cytochromes P450, flavin-monooxygenases, carboxyl­esterases, epoxide hydrolase, UDP-glu­cur­ono­syl­transferases and other drug-metabolizing enzymes.

Liver microsomes from humans and toxicologically relevant species (mice, rats, rabbits, dogs and monkeys) are widely used to evaluate species differences and similarities in metabolite formation (metabolic profiling). Microsomes from liver and small intestine are used to examine the potential for first-pass metabolism of orally administered drugs. Microsomes from small intestine, kidney and lung are often used to evaluate the potential for extrahepatic metabolism of a drug candidate.

XTreme 200 Pool: Our 200 donor human liver microsome pool.

Download a Sample XTreme 200 Datasheet Here!

Commercial large pool comparisons under same assay conditions:

Direct comparison of datasheets between XT and BD is misleading. XenoTech performs all CYP assays under the same experimental conditions, whereas BD Biosciences optimizes conditions for different enzymes by changing buffer composition and/or ionic strength, depending on the CYP enzyme. These differences in assay conditions influence the individual CYP activities. XenoTech assayed these large pools (XTreme 200 and BD’s pool of 150) side-by-side under the same conditions, and found only slight differences in CYP activity between the two pools.

Comparison of CYP enzyme activities in XenoTech's XTreme 200 HLM and BD Biosciences' pool of 150 HLM:

Measured levels of immunoreactive CYP protein vary widely depending on the choice of standard (recombinant or purified CYP enzyme) and the specificity of the antibody, as reported by Perrett et al., 2007). Western immunoblotting is semi-quantitative at best because the concentration-response curve for the standard is not the same as that for the corresponding protein in microsomes.

Packaging

Concentration: 20 mg/mL
Suspension buffer: 250 mM sucrose

Characterization Provided

Specific content of cytochrome P450
Specific content of cytochrome b5
NADPH-cytochrome c reductase activity
CYP1A2          Phenacetin O-dealkylation
CYP2A6          Coumarin 7-hydroxylation
CYP2B6          Bupropion hydroxylation
CYP2C8          Amodiaquine N-dealkylation
CYP2C9          Diclofenac 4´-hydroxylation
CYP2C19        S-Mephenytoin 4´-hydroxylation
CYP2D6          Dextromethorphan O-demethylation
CYP2E1          Chlorzoxazone 6-hydroxylation
CYP3A4/5       Testosterone 6β-hydroxylation
CYP3A4/5       Midazolam 1´-hydroxylation
FMO               Benzydamine N-oxygenation
UGT1A1          17β-estradiol 3-glucuronidation
UGT2B7          Morphine 3-glucuronidation
UGT1A6          1-Naphthyl glucuronidation
UGT1A9          Propofol glucuronidation
UGT1A4          Trifluoperazine glucuronidation

Donor information (age, ethnicity, gender, cause of death and infectious disease status)

Product Details

• XTreme 200 Pooled Human Liver Microsomes:
  • 100 male, 100 female
  • Km, Vmax and intrinsic clearance provided for each CYP
  • CYP activities determined with validated LC-MS/MS methods under uniform conditions
  • Study Manager, Study Director and QC review of data
  • S9 fraction and cytosol available from same donor pool
  • Large lots with reserve tissue from all 200 donors allow long-term availability
• Pooled Human Liver Microsomes
  • At least 50 donors
  • Pooled irrespective of gender or racial back­ground
  • Each sample significantly (but not necessarily equally) repre­sented in the pool
  • Offered in bulk amounts
    • 5 mL at 20 mg/mL
    • 50 mL at 20 mg/mL
    • 81 vial box, each vial 0.5mL @ 20mg/mL
  • Intended Use
    • Primarily for high-throughput screening of metabolic stability of drug candidates
    • Enzyme inhibition studies
    • Chemical and antibody inhibition experiments
    • Studies of species differences in drug metabolism
  • Donor information included with each order
• Pooled Male Human Liver Microsomes
  • At least 10 male donors
  • Each donor equally represented in the pool
  • Intended for in vitro studies of gender differences in drug metabolism
• Pooled Female Human Liver Microsomes
  • At least 10 female donors 
  • Each donor equally represented in the pool
  • Intended for in vitro studies of gender differences in drug metabolism
• CMV-Free Pooled Human Liver Microsomes
  • At least eight cytomegalovirus (CMV)-negative donors
  • Pooled irrespective of gender or racial back­ground
  • Each sample significantly (but not necessarily equally) represented in the pool
  • Primarily for high-throughput screening of metabolic stability of drug candidates

Related Products

• Individual Human Liver Microsome samples
  • Available upon request
  • Contact us for information
• Genotyped Human Liver Microsomes

Caution

In the case of human tissue, XenoTech accepts only non-transplantable tissue from donors who test negative for HIV 1 and 2, HTLV, and Hepatitis B and C. However, as a precaution, all human-de­rived samples should be regarded as a potential bio­hazard and should be stored, handled and discarded accordingly. Cellular and subcellular fractions are intended for in vitro use only.

Products

Product #	Name	Gender	Amount
H0604	CMV-Free Pooled Human Liver Microsomes	Mixed	0.5 mL at 20 mg/mL
H0610	Pooled Human Liver Microsomes	Mixed	0.5 mL at 20 mg/mL
H0610-81	Pooled Human Liver Microsomes- Box of 81	Mixed	81, 0.5mL vials @ 20.mg/mL
H0620	Pooled Human Liver Microsomes	Mixed	1.0 mL at 20 mg/mL
H0630	Pooled Human Liver Microsomes	Mixed	5.0 mL at 20 mg/mL
H0640	Pooled Human Liver Microsomes	Mixed	50 mL at 20 mg/mL
H1000	Pooled Human Liver Microsomes	Male	0.5 mL at 20 mg/mL
H1500	Pooled Human Liver Microsomes	Female	0.5 mL at 20 mg/mL
H2610	XTreme 200 Pooled Human Liver Microsomes	Mixed	0.5 mL at 20 mg/mL
H2610-81	XTreme 200 Pooled Human Liver Microsomes-Box of 81	Mixed	81, 0.5mL vials @ 20mg/mL
H2620	XTreme 200 Pooled Human Liver Microsomes	Mixed	1.0 mL at 20 mg/mL
H2630	XTreme 200 Pooled Human Liver Microsomes	Mixed	5.0 mL at 20 mg/mL
H2640	XTreme 200 Pooled Human Liver Microsomes	Mixed	50 mL at 20 mg/mL