rev:    5/15/2008

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CYTOCHROME P450

RECOMBINANT    ENZYMES 

(see also our special line of native enzymes)

see also below the recombinant human NADPH-P450 Oxidoreductase &  Cytochrome b5


Cytochrome P450,    Recombinant Human,  

Purified  & Purified Reconstituted Form ,or Microsomes       

-10% discount on 5 or more any combination   (except **) BULK QUOTES ON REQUEST

P450 Isoform               Product#             Format            Quantity          Price

     IA2                          RDI-P2294          Purified             150 ug             $375.00

     IA2                         RDI-P2304         Reconstituted (see below)      $562.00

     3A4                         RDI-P2194          Purified             150 ug             $375.00

     3A4                         RDI-P2305          Reconstituted (see below)        $1000.00 **

     3A4                         RDI-P2377          Microsomes     0.5nmol            $242.00
                                    new cat#: 30R-AC031

     3A5                         RDI-P2512          microsomes      0.5nmol            $242.00
                                    new cat#: 30R-AC033                        

     2C9                         RDI-P2355          Purified            100ug                $375.00

     2C9                         RDI-P2378          Microsomes    0.5nmol              $242.00
                                    new cat#: 30R-AC030

     2C9                         RDI-P2362         Reconstituted (see below)          $625.00

     2C19                       RDI-P2570          Microsomes      0.5nmol            $219.00

     2D6                         RDI-P2283          Microsomes      0.5nmol            $219.00

     2D6                         RDI-P2774           purified (*)      150ug               $375.00

     2E1                         RDI-P2223           Purified            150 ug              $412.50
                                    new cat#: 30R-AC037

     2E1                         RDI-P2306           Reconstituted (see below)        $1000.00 **

 P450 control               RDI-P2315           negative microsome control 5mg $242.00 **
                                    new cat#: 30R-AT014


Applications
* In vitro Drug Metabolism & toxicology Research

* Stereo-and/or Regio-specific Hydroxylation Reactions

Description

The hepatic microsomal cytochrome P450s are members of a superfamily of monoocygenases that catalyze the Phase I metabolism of xenobiotics, the initial step in the biotransformation and elimination of a wide variety of drugs and environmental pollutants.These P450s are located primarily in the liver and are integrated into the membrane of the endophasmic reticulum.The difficulty and tediousness of isolating and reconstituting the native enzymes from human tissue has hampered their use for drug metabolism studies with well-defined in vitro sytems. Recent development of methods for high level expression of active, mammalian P450s with baculovirus and E. coli has enabled RDI to offer recombinant human P450 isoforms in three different formats: Soluble purified enzymes, purified enzymes in a reconstituted format, and recombinant microsomes.

Soluble, purified, recombinant human P450s are produced in E.coli. All have been modified to some degree at the N-termainal to allow expression in E.coli, but these changes have not caused any discernible changes in substrate specificity or catalytic properties. The purified enzymes are available either as separatecomponents or in a reconstituted format with oxidoreductase, cytochrome b5, and the appropriate lipids, which offers the advantages of using highly purified enzymes. These microsomes are produced from insect cells coinfected with a baculovirus vector expressing both a P450 isoform and rabbit NADPH-P450 oxidoreductase. This format is very simple to use and requires no additional protein components for full enzymatic activity. The turnover numbers for P450s in both formates are similar to that seen using human liver microsomes.


Purified P450s in Reconstituted Form
RDI provides some purified P450s in a ready-to-use reconstituted form that includes a complete enzyme mix and separate reaction buffer. This "Mix and Metabolize" configuration greatly simplifies the use of purified cytochrome P450 isozymes with their associated protein, making them as easy to use as microsomes but with the inherent advantage of purified proteins. The amount of the three contained in the reconstituted format varies for each P450 isoform version. For example, the 3A4 reconstituted version contains a mixture of 3750 pmol, P450 protein, 7500 pmol NADPH-P450 oxidoreductase,and 3750 pmol cytochrome b5. In all cases, however, each version contains sufficient protein to perform 50-100 asays. The amount of enzyme mix and the volume used for an assay will depend on several factors which include:

The sensitivity of the analytical assay for the metabolites and products from catalysis, the kinetic parameter of enzyme catalysis for a particular substrate and P450 if known, the incubation period of the assay, the solubility of the test compound or substrate, or the specific preferences of individual research groups.

*Please note that some purified P450's  are available as either an individual purified isoform or with the isoform included in the easy-to-use Reconstituted Form. The reconstituted version contains two solutions: Solution 1: Enzyme Mix, which contains a mixture of recombinant P450 protein, NADPH-P450 oxidoreductase, and cytochrome b5 in an optimized buffer solution,and Soluation 2- The Reaction Buffer. A "Mix and Metabolize" protocol is also included with each kit. The amount of the three proteins contained in the reconstituted format varies for each P450 isoform version. For example, the P450 3A4 reconstituted version contains 3750 pmol P450 protein, 7500 pmol oxidoreductase, and 3750 pmol cytochrome b5. In all cases, however, each version contains sufficient protein to perform 50-100 assays, depending on the specific application.

CLICK HERE to View a sample protocol and references for using CYP's  in reconstituted form

Click here to view a sample protocol and references for using CYP's in microsome form.




SAMPLE SPECIFICATIONS: (see batch sheet with each shipment for batch specific information)

Cytochrome P450 Specifications:

Isoform 1A2

Format Purified *

Concentration: 0.8 mg/ml in 120 mM potassium phosphate pH 7.4, 0.1 mM EDTA, 0.05 mM DTT, 20% (v/v) glycerol

Guaranteed Amount of CYP450: > 1500 pmol

Specific Content: > 10 nmol spectral P450 per milligram of protein.

Source: Human recombinant protein produced from overexpressing plasmid in E.col. N-terminal modifications were as pre viously described (Sandhu et al. 1994, Arch.Biochem. Biophys. 309 168-177).

Specific Activity: Ethoxyresorufin: > 250 pmol/min/nmol    , Methoxyresorufin: > 500 pmol/min/nmol

Isoform  3A4

Format: Purified*

Concentration: >0.8 mg/ml in 20mM potassium phosphate pH 7.4,0.2

mM EDTA, 1mM DTT, 20% (v/v) glycerol

Guaranteed Amount of CYP450: > 1500 pmol

Specific Content: > 10 nmol spectral P450 per milligram of protein.

Source: Human recombinant protein produced from overexpressing plasmid in E.coli. N-terminal modifications were as previously described (Gillam et al. 1993,Arch.Biochem.Biophys. 305 123-131)

Specific Activity: Erythromycin: > 3 nmol/min/nmol,  Testosterone: > 12 nmol/min/nmol


Isoform: 3A4

Format: Microsomes

Concentration: > 20mg/ml in 100mM potassium phosphate pH 7.5,0.1 mM EDTA, 1mM DTT, 20% (v/v) glycerol.

Guaranteed Amount of CYP450: > 750 pmol

Specific Content: > 30 pmol spectral P450 per milligram of protein.

Source: Microsomes prepared from insect cells that were infected with a baculovirus containing the cDNA for human CYP3A4 and rabbit cytochrome P450 oxidoreductase (CYPOR).

Specific Activity: Testosterone: > 4.5 nmol/min/mg.


Isoform: 2C19

Format: Microsomes

Concentration: > 20 mg/ml in 100mM potassium phosphate pH 7.5.0.1 mM EDTA, 1mM DTT, 20% (v/v) glycerol.

Guaranteed Amount of CYP450: >2000 pmol

Specific Content: > 80 pmol spectral P450 per milligram of protein.

Source: Microsomes prepared from insect cells that were infected with a baculovirus containing the cDNA for human CYP3A4 and rabbit cytochrome P450 oxidoreductase (CYPOR)

Specific Activity: Mephenytoin: > 400 pmo/min/mg


Isoform: 2D6

Format: Microsomes

Concentration: >20 mg/ml in 100 mM potassium phosphate pH 7.5,0.1 mM EDTA, 1mM DTT, 20% (v/v) glycerol.

Guaranteed Amount of CYP450: >250 pmol

Specific Content: > 10 pmol spectral P450 per milligram of protein.

Source: Microsomes prepared from insect cells that were infected with a baculovirus containing the cDNA for human CYP2D6 (valine at position 374) and rabbit cytochrome P450 oxidoreductase (CYPOR).

Specific Activity: Bufuralol: > 1 nmol/min/mg.


Isoform: 2E1

Format: Purified*

Concentration: >0.8 mg/ml in 50 mM Tris HC1 pH 7.7,0.1 mM EDTA, 0.05 mM DTT. 20% (v/v) glycerol.

Guaranteed Amount of CYP450: > 1500 pmol.

Specific Content: > 10 nmol spectral P450 per milligram of protein.

Source: Human recombinant protein produced from overexpressing plasmid in E.coli. N-terminal modifications were as previously described (Gillam et.al. 1994, Arch.Biochem.Biophys. 312 59-66).

Specific Activity: N-Nitrosodimethylamine: > 8 nmol/min/nmol, Chlorzoxazone: > 5 nmol/min/nmol.



All isoforms should be stored at -80'C.


Additional DRUG METABOLIZING ENZYMES (for use with the above CYP450's)


DRUG METABOLIZING ENZYMES (REVISED) NEW HUMAN  Recombinant MATERIAL

Product  #          Source           Quantity      Price

P2309                HUMAN        200 ug       $375.00

-Bulk Quotes on request

NADPH-P450 Oxidoreductase Purified,Recombinant HUMAN

-replaces older discontinued rat material-

Applications

* For use with in vitro P450-dependent Biotransformation Reactions.

* In Vitro Drug Metabolism & Toxicology Research


Description

NADPH-P450 Oxidoreducatase (OR) transfers electrons form NADPH to the various isoforms of cytochrome P450; it is typically used at a 1:1 or 2:1 ratio to P450 for in vitro reconstitution assays. It is a membrane-bound flavoprotein, containing one mol each of FAD and FMN. The new RDI product is HUMAN Oxidoreductase produced from a recombinant baculovirus. . Also see our native human oxidoreductase.

Sample Specifications Source: Recombinant (insect cells infected with a   baculovirus)

Concentration: 1.2mg/ml in 10mM potassium phosphate, pH 7.7, 0.1 mM EDTA, 1mM DTT ,20% glycerol.

Physical Purity: Greater than 90% as assessed by visualization of   5 ug of protein on Coomassic-stained SDS gel

Activity: 24 umol cytochrome c reduced per minute per milligram protein at room temperature. Using a MW of

76.5 kDa, 6.4ul=100 pmoles.

Storage: -80 DEG C long term. Avoid repeated freeze thaw cycles.

 

References

1. Yamano,S.,Aoyama,T.,McBride,O.W.,Hardwick,J.P.,Geiboin,H.V., Gonzalez,F.J.,(1989) Molec.Pharmacol 35: 83-88

2. Schenkman,J.,Greim,H.,eds.(1993) Handbook of Experimental Pharmacology, vol. 105.

3. Shen,A.L., Porter,T.D., Wilson,T.E., and Kasper,C.B.,(1989) J. Biol,Chem. 264: 7584-7589


CYTOCHROME b5

Product#               Source           Quantity          Price

RDI-P2252           Human             100 ug          $412.50
new cat#: 30R-AC036

Applications

* For use with in vitro P450-dependent Biotransformation Reactions

* In Vitro Drug Metabolism & Toxicology Research.


Description

Cytochrome b5 is a membrane-bound hemoprotein that enhances the catalytic efficiency of some P450 isoforms,most notably members of the 3A subfamily/ It is not clear whether it plays a direct role in electron transfer or an indirect role through allosteric interactions with the P450. RDI Cytochrome b5 is overexpressed from the human cDNA in E. coli, purified to homogeneity, and supplied in a soluble format. Quality control includes testing theability of the enzyme to stimulate testosterone 6B-hydroxylation in a  reconstituted system with human P450 3A4. See also our native expressed cytochrome b5.


Specifications

Source: Recombinant E. coli.

Concentration: 0.5-10 mg/ml

Physical Purity: Greater than 90% as assessed by visualization of 10 mg of protein on a Coomassie-stained SDS

Quantitation: Heme content measured using difference spectrophotomctry. An extinction coefficient of gel 118 mM-1 cm-1 for the absorbance difference between 490 and 424 nm is used to calculate the concentration of Cytochrom b5


References:

1. Gillam,F.M.J., Baba,T.,Kim,B.R.,Ohmon,S., Guengerich,F.P.,(1993) Arch. Biochem.Biophys. 305: 123-131

2. Holomans,P.J. Shet.M.S. Marion-Wixtrom,C.A.,Fisher,C.W., Estabrook,R.W. (1994) Arch.Biochem,Biophys.312:554-565.


Precaution: For in vitro research use only-not for use in or on humans or animals-not for use in diagnostics. Not responsible for any patent infringements with the use or derivation of these products.

See also our various antibodies for use with many of the native and recombinant CYP450's


RDI Division of Fitzgerald Industries Intl

34 Junction Square Drive

Concord MA 01742-3049

USA

phone (800) 370-2222 or

          (978) 371-6446 or (800) 370-2222

fax     (978) 371-2266

EMAIL:antibodies@fitzgerald-fii.com

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