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Your metabolic tools for drug discovery & development GIBCO® microsomes & other liver subcellular fractions

  • Large pooled lots for reproducible, long-term studies
  • Fractions carefully isolated by experts in hepatic biology
  • Microsomes functionally tested for select CYP450 and Phase II enzyme activities

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Human microsome pools and subcellular fractions

Subcellular fractions, derived from the endoplasmic reticulum of liver, contain a rich variety of metabolic enzymes for assessing the in vitro metabolism of drug candidates (Table 1) and are suitable for a variety of experiments:

  • Cytochrome P450 inhibition studies
  • Metabolic stability
  • Cytochrome P450 phenotyping
  • Metabolite characterization


50 donor human liver microsome pool
Designed to maximize functionality for all your study types- suitable for inhibition, clearance, or metabolic identification.

  • Equal representation of all 50 donors
  • Activities representing the typical patient population


11 specialty human liver microsome pools
Prepared with 5 to 20 donors each and pooled for your convenience according to age, gender, body mass index, high 3A activity, and high 2D6 activity.

Customized microsome pools
Our scientists will create a customized pool specifically for your unique research needs using our large, fully characterized single-donor database.

Life Technologies provides liver subcellular fractions from a variety of tox species, including human, nonhuman primates (Cynomolgus Monkey and Rhesus Monkey), dog (Beagle), rat (Sprague-Dawley), mouse (CD-1),  and trout (Oncorhynchus mykiss).  Custom species are available upon request. 

Each product contains an average representative pool of donors.  Human microsome pools are fully characterized (Km and Vmax) according to GLP standards for major cytochrome P450 activities and select Phase II enzymes using FDA recommended substrates (Tables 2-3).

Table 1 - Relevant applications for liver subcellular fractions


Metabolic  Enzymes Liver Microsomes Liver S9 Fractions Liver Cytosol
Aldehyde Oxidase

X
X
Cytochromes P450 (CYP)X
X

Flavin Monooxygenases (FMO)
X
X

Glutathione Transferase (GST)
X

Monamine Oxidase (MAO)

X

Sulfurotrnasferase (SULT)

X
X
Uridine Glucuronide Transferase (UGT)
X
X

Table 2 - Cytochrome P450 and Phase II enzymes tested in GIBCO® human microsome pools


Enzyme Monitored Marker Substrate Incubation (min) Protein Concentration (mg/ml) Metabolite
CYP1A1/2
Phenacetin
30
0.1
Acetaminophen
CYP2A6
Coumarin
5
0.025
7-Hydroxycoumarin
CYP2B6
Bupropion
20
0.25
Hydroxybupropion
CYP2C8
Paclitaxel
10
0.075
6α-Hydroxypaclitaxel
CYP2C9
Tolbutamide
20
0.1
Hydroxytolubutamide
CYP2C19
(S) Mephenytoin
30
0.1
4'-Hydroxymephenytoin
CYP2D6
Dextromethorphan
15
0.2
Dextrorphan
CYP2E1
Chlorzoxazone
20
0.1
6-Hydroxychlorzoxazone
CYP3A4/5
Midazolam4
0.025
1'-Hydroxymidazolam
CYP3A4/5
Testosterone7
0.05
6β-Hydroxytestosterone
CYP4A11
Lauric Acid
15
0.2
12-Hydroxydecanoic Acid
FMO
Methyl p-Tolylsulfide15
0.05
Methyl p-Tolylsulfide
UGT
7-Hydroxycoumarin
30
0.2
7-Hydroxycoumarin Glucuronide

Table 3 - Kinetic parameters for the GIBCO® 50 donor human liver microsome pool


Isoform Metabolite Km(μM) Vmax (nmol/min/mg)
CYP1A2Acetaminophen780.73
CYP2A67-Hydroxycoumarin1.10.53
CYP2B6Hydroxybupropion640.29
CYP2C86α-Hydroxypaclitaxel5.50.15
CYP2C9Hydroxytolbutamide2200.19
CYP2C194'-Hydroxymephenytoin340.031
CYP2D6Dextrophan3.20.13
CYP2E16-Hydroxychlorzoxazone701.4
CYP3A46β-Hydroxytestosterone194.0
CYP3A41'-Hydroxymidazolam1.61.1

Ordering Is Simple!

To call in orders please use the following information:

Asia-Pacific Sales:
Tel:  866.952.3559
Fax: 866.902.3559
Email:  hepaticproducts@invitrogen.com

Invitrogen Japan Sales:
Tel:  +81 3 5566 6160
Fax:  +81 3 5566 6505

or order by email at jpinfo@invitrogen.com

Product Concentration Quantity Cat. No. Price
Human microsomes, 50 donors20 mg/ml0.5 mlHMMC-PL050$105
Dog (beagle) microsomes20 mg/ml0.5 mlDGMC-PL$60
Monkey (cynomolgus) microsomes20 mg/ml0.5 mlMKMC-PL$120
Mouse (Balb/c) microsomes20 mg/ml0.5 mlMSMC-PL$45
Rat (Sprague-Dawley) microsomes20 mg/ml0.5 mlRTMC-PL$35
Human S9 fractions, pooled20 mg/ml1.0 mlHMS9-PL$85
Dog (beagle) S9 fractions20 mg/ml1.0 mlDGS9-PL$65
Monkey (cynomolgus) S9 fractions20 mg/ml1.0 mlMKS9-PL$80
Mouse (CD-1) S9 fractions20 mg/ml1.0 mlMSS9-PL$45
Rat (Sprague-Dawley) S9 fractions20 mg/ml1.0 mlRTS9-PL$35
Fish (rainbow trout) S9 fractions20 mg/ml1.0 mlTRS9-PL$60
Human cytosol, pooled20 mg/ml1.0 mlHMCY-PL$45
Dog (beagle) cytosol20 mg/ml1.0 mlDGCY-PL$40
Monkey (cynomolgus) cytosol20 mg/ml1.0 mlMKCY-PL$60
Mouse (CD-1) cytosol20 mg/ml1.0 mlMSCY-PL$40
Rat (Sprague-Dawley) cytosol20 mg/ml1.0 mlRTCY-PL$30

For Research Use Only. Not for use in diagnostic procedures.