Subtitle: ADME/Tox Intelligence, DDI Risk Assessment, and High-Purity Reagents for Phase II Metabolism Studies.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for UGT1A4 drug discovery and drug-drug interaction (DDI) screening. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen | UGT1A4 Recombinant Membrane Protein, HEK293-derived microsomal fraction, >95% purity (SDS-PAGE), Sequence Verified, Endotoxin <1 EU/µg. | View UGT1A4 Products |
| Gene Delivery | UGT1A4 ORF Lentivirus, CMV promoter, Puromycin selection marker, for stable HepG2/HEK293 metabolic cell lines. | View UGT1A4 Products |
| Benchmark Ab | Anti-UGT1A4 Antibody, Recombinant positive control for immunoblotting. | View UGT1A4 Products |
| Validator | UGT1A4 siRNA Set, Three pre-designed sequences for knockdown validation via RT-qPCR. | View UGT1A4 Products |
| Related Target A | UGT1A1 – Bilirubin metabolism; critical for selective vs. overlapping substrate screening. | View UGT1A1 Products |
| Related Target B | CYP3A4 – Synergistic Phase I metabolism network. | View CYP3A4 Products |
| Related Target C | UGT2B7 – Major opioid/NSAID metabolizing isoform; essential for cross-isoform inhibition assays. | View UGT2B7 Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| Subfamily counter screening (UGT1A1 vs 1A4) | Homolog panel proteins strictly verified by mass spec and sequence analysis. |
| Complex Membrane Localization (ER) | Lentivirus premade particles for stable hepatocyte cell line construction; HEK293 Microsomal Fractions retaining native ER membrane association. |
| Lack of Controls | Recombinant Benchmark Antibodies included for immunoblotting. |
| False Positives in Toxicity | Validated siRNA included for specificity checks. |
| Isoform-selective inhibition profiling | Homolog Panel available: UGT1A1, UGT1A3, UGT1A6, UGT2B7 proteins strictly verified by sequence alignment. |
| Reproducible kinetic parameters (Km/Vmax) | Endotoxin Controlled (<1 EU/µg) to eliminate LPS interference in cellular co-incubation assays. |
Key Genetic Variants
UGT1A4 harbors several clinically relevant polymorphisms that influence drug metabolism:
- rs3892221 (UniProt VAR_059844)
- rs6755571 (UniProt VAR_024684)
- rs2011425: increases glucuronosyltransferase activity towards calcidiol (UniProt VAR_058584)
These variants are critical for pharmacogenomic testing and personalized dosing of substrates such as lamotrigine and olanzapine.
Live UGT1A4 R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Global Clinical Landscape & Future Outlook
Regulatory scrutiny on Phase II metabolism is intensifying as the FDA and EMA update guidelines for Drug-Drug Interaction (DDI) studies. UGT1A4, a major Phase II drug-metabolizing enzyme, is responsible for the glucuronidation of numerous therapeutic amines and steroids, including lamotrigine, olanzapine, and trifluoperazine. Regulatory agencies increasingly require comprehensive UGT phenotyping to predict DDIs and clearance rates. As precision medicine advances, the next wave of R&D is highly focused on pharmacogenomic variants of UGT1A4 to understand patient-specific metabolic profiles. The shift toward personalized medicine is driving demand for UGT phenotyping and genotyping assays, while complex biologics (ADCs, bispecifics) require deeper metabolic characterization beyond CYP450 pathways.
Competitive Modality & Indication Snapshot
| Modality | Focus / Application | Key Substrates / Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Small Molecule | Global CROs, Preclinical Pharma | Pan-indication ADME/Tox | Enzymatic Assay (Need high-purity recombinant enzymes) |
| Targeted Protein Degradation | Biotechs | Oncology, Autoimmune | Clearance Validation (Need stable UGT1A4 cell lines via Lentivirus) |
| Pharmacogenomics | Diagnostic Developers | Personalized Medicine | Variant Screening (Need Mutant Recombinant Proteins) |
| Recombinant Enzyme Assay | In vitro DDI Screening (FDA Guidance) | Lamotrigine, Olanzapine | High-purity membrane protein with preserved activity |
| Stable Cell Line | Metabolic Stability (t½ prediction) | Trifluoperazine, Asenapine | Lentivirus for stable overexpression in hepatocytes |
| Genotyping Reference | Pharmacogenomic Testing | UGT1A42, UGT1A43 variants | Wild-type vs. mutant protein comparison kits |