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Cell4Pharma ABC Transporter Vesicle Kits

HEK293-derived inside-out membrane vesicle kits for the full panel of regulatory ABC transporters — BSEP, BCRP, P-gp and MRP1–MRP5/MRP8 — for DDI studies and DILI risk assessment per FDA and EMA guidance.

Cell4Pharma ABC Transporter Vesicle Kits, SeamlessBio
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Full Regulatory Panel

BSEP, BCRP, P-gp and MRP1–MRP5/MRP8 — the complete set of transporters referenced in FDA and EMA DDI guidance.

02

100 Reactions per Kit

Each kit is sized for 100 reactions in a 96-well plate format, suitable for IC50 determination and screening.

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Inside-Out HEK293 Vesicles

Confirmed transporter expression and orientation for reliable, reproducible transport data.

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Assay Service Available

Don't have in-house capacity? Our ciPTEC assay service can run the full transporter panel for you.

Kit specifications and guaranteed transport ratios

Every kit is released against a validated probe substrate with a specified minimum ATP/AMP transport ratio.

The ATP/AMP ratio is the practical quality metric for a vesicular transport assay. It expresses how much of the measured accumulation is genuine ATP-dependent transport rather than passive uptake and non-specific binding. A low ratio compresses the assay window and inflates IC50 variability — which is why it belongs on the datasheet rather than in the small print.

TransporterProbe substrateATP/AMP ratio
P-gp (MDR1, ABCB1)Convallatoxin> 5
BSEP (ABCB11)Taurocholate (TCA)> 10
BCRP (ABCG2)Estrone-3-sulfate (E1S)> 10
MRP1 (ABCC1)Estradiol-17β-glucuronide> 5
MRP2 (ABCC2)CDCF> 10
MRP3 (ABCC3)Estradiol-17β-glucuronide> 10
MRP4 (ABCC4)DHEAS> 5
MRP5 (ABCC5)CDCF> 3
MRP8 (ABCC11)DHEAS> 3

Lot-specific activity data is supplied with each kit. Control vesicles from non-transfected HEK293 cells are available separately and belong in every assay run — ATP-dependent transport is defined as the difference between the two.

Format and handling

HEK293Human expression system, not Sf9 insect cells
100Reactions per vial
≥ 1 yearStorage at −80 °C
0Cell culture steps before use
  • Ready on thawing. No expansion, no differentiation, no monolayer to qualify — the vesicles go straight from −80 °C into the assay.
  • Robust to handling. Transport activity is retained after storage at −20 °C, after two days at 4 °C, and across five freeze-thaw cycles.
  • Detection-agnostic. Compatible with radiolabel, LC-MS/MS and fluorescence readouts — see the detection method comparison.
  • EU stock. Supplied from Europe for the DACH region — no US import lead time or customs delay.
Why HEK293 and not Sf9: ABC transporters are glycosylated mammalian membrane proteins. Host cell choice determines post-translational modification and membrane lipid composition, and both affect transport kinetics. A human expression system removes a variable that an insect cell system introduces. The full argument is in HEK293 vs. Sf9 vesicles.

Why ABC transporter testing matters in DMPK programs

ABC (ATP-binding cassette) transporters mediate the efflux of drugs and metabolites across cell membranes, and inhibition of key transporters — particularly BSEP, BCRP and P-gp — is mechanistically linked to drug-induced liver injury (DILI) and clinically relevant drug-drug interactions (DDI). FDA and EMA guidance both recommend transporter inhibition testing as part of standard DMPK characterisation.

The vesicle-based assay format uses HEK293-derived inside-out membrane vesicles with confirmed transporter expression, allowing direct measurement of transporter-mediated substrate uptake in the presence and absence of test compounds — the basis for IC50 determination and single-concentration screening.

Because inhibition of multiple transporters can compound DILI risk — for example, BSEP inhibition together with MRP2, MRP3 or MRP4 impairs the compensatory bile acid efflux pathways that partially protect hepatocytes — a full panel typically gives a more complete risk picture than testing BSEP in isolation.

Typical applications

  • Drug-induced liver injury (DILI) risk assessment
  • Drug-drug interaction (DDI) studies per FDA/EMA guidance
  • Hepatotoxicity screening in lead optimisation
  • IC50 determination for transporter inhibitors
  • Regulatory submission transporter panels
  • Academic and pharmaceutical DMPK research
Products

ABC Transporter Vesicle Kits — Overview

Choose the transporter kit matched to your study. Bulk pricing and full panel quotes are available on request.

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