GeneBLAzer® Validated Assays for Nuclear Receptors (NRs) provide you with a reliable, rapid, and sensitive method for analyzing the intracellular status of NRs upon exposure to drug candidates or other stimuli. These functional assays allow for measurement of receptor activation or inhibition by compounds and can be used to determine compound potency and selectivity.

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All GeneBLAzer® Validated Assays provide superior response profiles as a result of response element optimization and use of optimal clones. GeneBLAzer® Validated Assays for NRs:
  • Provide ready-to-screen, ratiometric assays for disease relevant NR targets
  • Are functionally validated to ensure high-quality results each and every time
  • Can be designed with your desired target and cell line through our Custom Assay Services program.

GeneBLAzer® Validated Assays for NRs are tested and documented to show a high level of performance. These assays are shown to meet the following specifications:
  • Z’-factor of >0.6
  • Appropriate EC50 responses to known agonists and antagonists
  • Mycoplasma negative
  • DMSO tolerance up to 1%
  • Optimized stimulation time, cell density, and substrate loading times

GeneBLAzer® Validated Assays for Nuclear Receptors Mechanism of Action

 GeneBLAzer Validated Assays

GeneBLAzer® Nuclear Receptor Assays use a β-lactamase cDNA under transcriptional control of an Upstream Activator Sequence (UAS). The UAS is activated by the GAL4 transcription factor (DNA binding domain), which is expressed as a fusion protein with the target receptor ligand binding domain. Upon ligand binding, the GAL4(DBD)-NR(LBD) fusion protein translocates to the nucleus, where it binds to the UAS which controls transcription of β-lactamase.

GeneBLAzer® Validated Assays for Nuclear Receptors Select Validation Data

Dose response curves for a panel of known agonists are shown in the GeneBLAzer® ERB Assay. The rank order of potency of these agonists is consistent with known literature values.
 GeneBLAzer Known Agonists
Dose response curves of a panel of partial agonist/antagonist compounds are shown in the ERB Assay, and the results are consistent with known literature values. These compounds are partial agonists as well as antagonists for Era, but only antagonists for ERB. For antagonist mode, cells were tested in the presence of EC80 amounts of estradiol.
GeneBLAzer Partial Agonist Antagonist

Ordering Information

Sku Name Size Price Qty
K1698 GeneBLAzer® AR-UAS-bla Griptite™ Cells 2 x 10^6 cells USD 9,880.00
K1688 GeneBLAzer® ERα-UAS-bla GripTite™ Cells 2 x 10^6 cells USD 9,880.00
K1393 GeneBLAzer® ER Alpha DA Assay Kit 1 plate USD 996.00
K1702 GeneBLAzer® ERRα-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1421 GeneBLAzer® ERR Alpha DA Assay Kit 1 plate USD 996.00
K1691 GeneBLAzer® FXR-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1397 GeneBLAzer® FXR DA Assay Kit 1 plate USD 996.00
K1687 GeneBLAzer® GR-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1391 GeneBLAzer® GR DA Assay Kit 1 plate USD 996.00
K1692 GeneBLAzer® LXRα-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1401 GeneBLAzer® LXR alpha DA Assay Kit 1 plate USD 996.00
K1699 GeneBLAzer® LXRβ-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1415 GeneBLAzer® LXR beta DA Assay Kit 1 plate USD 996.00
K1696 GeneBLAzer® MR-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1409 GeneBLAzer® MR DA Assay Kit 1 plate USD 996.00
K1693 GeneBLAzer® PR-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1403 GeneBLAzer® PR DA Assay Kit 1 plate USD 996.00
K1690 GeneBLAzer® PPARδ-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1395 GeneBLAzer® PPAR delta DA Assay Kit 1 plate USD 996.00
K1419 GeneBLAzer® PPAR gamma DA Assay Kit 1 plate USD 996.00
K1685 GeneBLAzer® RARα-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1387 GeneBLAzer® RAR alpha DA Assay Kit 1 plate USD 996.00
K1695 GeneBLAzer® RARβ-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1407 GeneBLAzer® RAR-beta DA Assay Kit 1 plate USD 996.00
K1763 GeneBLAzer® RARγ-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1559 GeneBLAzer® RAR-gamma DA Assay Kit 1 plate USD 996.00
K1697 GeneBLAzer® RXRα-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1411 GeneBLAzer® RXR alpha DA Assay Kit 1 plate USD 996.00
K1694 GeneBLAzer® RXRβ-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1405 GeneBLAzer® RXR beta DA Assay Kit 1 plate USD 996.00
K1684 GeneBLAzer® TRα-UAS-bla HEK 293T Assay Kit 1 plate USD 9,880.00
K1385 GeneBLAzer® TR alpha DA Assay Kit 1 plate USD 996.00
K1686 GeneBLAzer® TRβ-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1389 GeneBLAzer® TR beta DA Assay Kit 1 plate USD 2,408.40
K1700 GeneBLAzer® VDR-UAS-bla HEK 293T Cells 2 x 10^6 cells USD 9,880.00
K1417 GeneBLAzer® VDR DA Assay Kit 1 plate USD 996.00
K1875 GeneBLAzer® PPAR alpha UAS-bla HEK 293T Cellular Assay Kit 2 x 10^6 cells USD 1,079.08