Human Liver Microsomes
View ProductsHuman liver
microsomes are widely used in drug discovery and preclinical drug development to evaluate the metabolism of drug candidates.
DESCRIPTIONPACKAGINGCHARACTERIZATION PROVIDEDPRODUCT DETAILSRELATED PRODUCTSSAFETY, HANDLING AND STORAGEPRODUCTSDESCRIPTION
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 phenotyping 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.
Return to TopPACKAGING
Concentration: 20 mg/mL
Suspension buffer: 250 mM sucrose
Return to Top CHARACTERIZATION PROVIDED
Specific content of cytochrome P450 |
Specific content of cytochrome b5 |
NADPH-cytochrome c reductase activity |
CYP1A2 |
Phenacetin O-dealkylation |
CYP1A2 |
Ethoxyresorufin 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 |
CYP4A11 |
Lauric acid 12-hydroxylation |
FMO |
Benzydamine N-oxidation |
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) |
Return to TopPRODUCT DETAILS
- 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
- 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
Return to Top - Individual Human Liver Microsome samples
- Genotyped Human Liver Microsomes
Return to TopSAFETY, HANDLING AND STORAGE
Informed Consent Statement
A single organization regulates and oversees the use of human tissue intended for transplantation in the United States, namely the United Network for Organ Sharing (UNOS). Organ donors may elect to have their organs used either for transplantation only, or for transplantation or research. Thus, the donor (or the donor's family) has the right to prevent the use of the donor's organs for research. Regardless of the use of donated organs, no compensation is given to the donor’s family; any such compensation is illegal in the United States. In those cases where donors (or family members) elect to withhold organs from research uses, any organs that cannot be transplanted are discarded.
XenoTech receives hepatic, renal, intestinal, pulmonary, and other human tissue from various regional organ procurement organizations (OPOs) that obtain organs approved for research use. Regulations in the United States require that, regardless whether the organ is intended for transplantation or research purposes, the organ donor's identity be treated as highly confidential information. Organ procurement organizations maintain the informed consent records from each donor, and our Standard Operating Procedure requires that XenoTech personnel confirm the existence of informed consent for research purposes, prior to transport of organs to XenoTech. This procedure is intended to ensure that XenoTech manufactures human-derived products only when informed consent has been granted for research use of those specific organs. XenoTech does not, and, in consideration of confidentiality, cannot obtain the informed consent records from these organizations.
All human tissue accepted by XenoTech has been tested for the possible presence of various infectious diseases, and XenoTech does not accept human-derived material unless the donor has tested negative (non-reactive) for RPR, HIVAb, HTLVAb, HBsAg and HCVAb. All human tissue is also tested for CMVAb. However, due to the widespread (nearly ubiquitous) appearance of CMV in the population, and its relative insignificance as an infectious agent, tissues from donors reactive for CMVAb are accepted. The serology status of each donor is typically determined by ELISA by the organ procurement hospital.
XenoTech does not deal directly with - nor does it make any direct payments to - the surgeons who procure organs or the medical institutions where they work.
Human liver microsomes should be stored in an ultra-low freezer (-70°C or colder). At ultra-low temperatures, XenoTech’s human liver microsomes are stable for several years, as reported by
Pearce et al.R. Pearce, C.J. McIntyre, A. Madan, U.Sanzgiri, A.J. Draper, P. Bullock, D.C. Cook, L.A. Burton, J. Latham, C. Nevins, and A. Parkinson. Effects of freezing, thawing, and storing human liver microsomes on cytochrome P450. Arch. Biochem. Biophys. 331, 145-169, 1996
Freezing and thawing samples
XenoTech’s human liver microsomes can be frozen and thawed as many as ten times with no apparent loss of P450 activity, as reported by Pearce et al. (cited above). Consequently, after an aliquot of human liver microsomes is taken from a vial, the residual sample can be re-frozen and stored at -70°C or below for later use. Care should be taken to keep thawed samples on ice (4°C), and to return them as quickly as possible to an ultra-low freezer for storage.
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.
Return to TopPRODUCTS
Product No. |
Product |
Gender |
Amount |
H0610 |
Pooled Human Liver Microsomes |
Mixed |
0.5 mL at 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 |
H0604 |
CMV-Free Pooled Human Liver Microsomes |
Mixed |
0.5 mL at 20 mg/mL |
Return to TopOrder Fax: 913.227.7171
Order E-mail: info@xenotechllc.com
Call 877.588.7530 (toll-free US and Canada) for pricing and availability.
If ordering outside of North America, please see our Distributor information.