Corning TransportoCells HEK293-derived ABC transporter vesicles express more human-like transporter proteins within the human cellular membrane. These HEK membrane vesicles have demonstrated a significantly higher uptake activity and lower background as compared with traditional insect cell-derived vesicles. The validated vesicle model could potentially improve in vitro to in vivo prediction because of the more in vivo-like recombinant proteins and membrane composition. The products can be used for drug transporter phenotyping, drug-drug interaction and toxicity studies, drug clearance prediction, and mechanistic studies of drug transport.

Contain more in vivo-like recombinant proteins and membrane composition, thus providing the potential for a better in vitro to in vivo correlation

Demonstrate a robust dynamic range with significantly higher uptake activity and lower background than insect cell expression systems

Has been fully validated for substrate specificity, transporter kinetics, and inhibition profiles

Support the USFDA, EMA, and ITC recommendations for the identification of drug transporters and transporter drug-drug interaction studies

Product Number

453801

Qty./Pk

1?/ Pk

Qty./Cs

1?/ Ea

Brand

Corning?

Species

Human

Protein Concentration

5 mg/mL

Transporter

MDR1/P-gp

Shelf Life

5 years

Storage

-80 C

Recombinant enzyme prepared from insect cells infected with baculovirus containing human UGT2B17 cDNAs

UDP-glucuronosyltransferases (UGT) represent the major phase II drug metabolism pathway in human. UGT enzymes catalyze the transfer of glucuronic acid (derived from UDPGA co-factor) to xenobiotics and endogenous substrates having nucleophilic acceptor groups, making them more polar and readily excreted in urine or bile. To date, at least 18 human UGT enzymes have been cloned and sequenced. Like the P450 enzymes, UGTs possess broad and overlapping substrate specificities. Clinically relevant drug interactions have been identified for UGT isoforms, leading regulatory agencies (FDA) to require drug interaction testing for compounds showing significant UGT metabolism.

UGT2B17 expressed in the liver as well as extra-hepatic tissues. Steroids, e.g. androsterone dihydrotestosterone, and testosterone have been shown to be substrates for UGT2B17.

Available size: 0.5 mL

Protein concentration: 5 mg/ mL

Product Number

456437

Qty./Pk

1?/ Pk

Qty./Cs

1?/ Ea

Brand

Corning?

Size

0.5 mL

Species

Human

Enzyme Type

UGT

Protein Concentration

5 mg/mL

Storage

-80 C

Cellular Location

Microsome

Recombinant enzyme prepared from insect cells infected with baculovirus containing desired cDNAs

CYP2A6 is the major coumarin 7-hydroxylase, which is a probe substrate activity for CYP2A6 in HLMs. CYP2A6 is the primary enzyme for nicotine clearance catalyzing the initial C-oxidation and subsequent cotinine hydroxylation step. CYP2A6 catalyzes the bioactivation of Tegafur to 5-fluorouracil, an anticancer agent.

CYP2A6 is inhibited by high ionic strength buffers. CYP2A6 is a low affinity enzyme for the activation of N-nitrosodimethylamine and a relatively high affinity enzyme for the activation of N-nitrosodiethylamine. CYP2A6 is a low affinity enzyme for the activation of aflatoxin B? and is also capable of activating benzo(a)pyrene and the tobacco smoke-derived nitrosamine, NNK.

Contains Human Oxidoreductase, but not cytochrome b?

Available size: 1.0 nmole P450 in 0.5 mL

Protein concentration: Available in batch data sheet. Contact Corning Scientific support to obtain the information.

Product Number

456204

Qty./Pk

1?/ Pk

Qty./Cs

1?/ Ea

Brand

Corning?

Size

1 nmol

Species

Human

Enzyme Type

P450

Protein Concentration

Lot-dependent

Storage

-80 C

Cellular Location

Microsome

Recombinant enzyme prepared from insect cells infected with baculovirus containing desired cDNAs

CYP2B6 is variably expressed in HLMs. CYP2B6 is involved in the metabolism of several drugs which include bupropion, efavirenz, S-mephenytoin (N-demethylation), and the anesthetics methoxyflurane and propofol. The structurally-related anticancer drugs cyclofosphamide and ifosfamide are activated by CYP2B6. CYP2B6 is capable of activating carcinogens such as aflatoxin B? and the tobacco smoke-derived nitrosamine, NNK, to the cytotoxic species. CYP2B6 protein levels can be induced several fold in the liver by ligands of CAR and PXR receptors (e.g. phenobarbital, rifampin, and phenytoin).

Contains Human Oxidoreductase and cytochrome b?

Available size: 0.5 nmole P450 in 0.5 mL

Protein concentration: Available in batch data sheet. Contact Corning Scientific support to obtain the information.

Product Number

456255

Qty./Pk

1?/ Pk

Qty./Cs

1?/ Ea

Brand

Corning?

Size

0.5 nmol

Species

Human

Enzyme Type

P450

Protein Concentration

Lot-dependent

Storage

-80 C

Cellular Location

Microsome

Corning? Supersomes? Human CYP2C19 + Oxidoreductase, 0.5 enzyme prepared from insect cells infected with baculovirus containing desired cDNAs

CYP2C19 metabolizes 5-10% of prescribed medications. CYP2C19 drug substrates include omeprazole, lansoprazole, pantoprazole, phenytoin, diazepam, and S-mephenytoin (4 -hydroxylation, probe substrate/activity). CYP2C19 is responsible for the (S)-mephenytoin 4 -hydroxylase polymorphism. Approximately 20% of Asians are deficient in CYP2C19 activity (due to two prevalent allelic variants: *2 and *3, which result in inactive protein.

Contains Human Oxidoreductase, but not cytochrome b?

Available size: 0.5 nmole P450 in 0.5 mL

Protein concentration: Available in batch data sheet. Contact Corning Scientific support to obtain the information.

Product Number

456219

Qty./Pk

1?/ Pk

Qty./Cs

1?/ Ea

Brand

Corning?

Size

0.5 nmol

Species

Human

Enzyme Type

P450

Protein Concentration

Lot-dependent

Storage

-80 C

Cellular Location

Microsome

This microsomes product is prepared from sexually mature male Gottingen pig livers and characterized for relevant cytochrome P450 enzyme activities.

Features/Benefits:

Poole liver microtomes prepared from sexually mature male Gottingen pigs

high manufacturing standards to reduce lot-to-lot variability and to ensure reproducibility

Available Size: 0.5 mL

Protein Concentration: 20 mg/ mL in 250 mM Sucrose

Shelf life: N/A (this product is stable for more than 10 years when stored properly)

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452322

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Corning?

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20 mg/mL

-80 C

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Recombinant enzyme prepared from insect cells infected with baculovirus containing desired cDNAs

CYP2B6 is variably expressed in HLMs. CYP2B6 is involved in the metabolism of several drugs which include bupropion, efavirenz, S-mephenytoin (N-demethylation), and the anesthetics methoxyflurane and propofol. The structurally-related anticancer drugs cyclofosphamide and ifosfamide are activated by CYP2B6. CYP2B6 is capable of activating carcinogens such as aflatoxin B1 and the tobacco smoke-derived nitrosamine, NNK, to the cytotoxic species. CYP2B6 protein levels can be induced several fold in the liver by ligands of CAR and PXR receptors (e.g. phenobarbital, rifampin, and phenytoin).

Contains Human Oxidoreductase, but not cytochrome b?

Available size: 0.5 nmole P450 in 0.5 mL

Product Number

456210

Qty./Pk

1?/ Pk

Qty./Cs

1?/ Ea

Brand

Corning?

Size

0.5 nmol

Species

Human

Enzyme Type

P450

Protein Concentration

Lot-dependent

Storage

-80 C

Cellular Location

Microsome

Protein concentration: Available in batch data sheet. Contact Corning Scientific support to obtain the information.

Recombinant enzyme prepared from insect cells infected with baculovirus containing desired cDNAs

CYP4F12 is expressed in both the liver and the intestine. It was shown that this enzyme is active for the hydroxylation of certain non-sedative antihistamines such as ebastine, astemizole and terfenadine.

Contains Human Oxidoreductase and cytochrome b?

Available size: 0.5 nmole P450 in 0.5 mL

Protein concentration: Available in batch data sheet. Contact Corning Scientific support to obtain the information.

Product Number

456275

Qty./Pk

1?/ Pk

Qty./Cs

1?/ Ea

Brand

Corning?

Size

0.5 nmol

Species

Human

Enzyme Type

P450

Protein Concentration

Lot-dependent

Storage

-80 C

Cellular Location

Microsome