Market Intelligence, Clinical Progress, and High-Purity Reagents for Metabolic Disease & NASH Development.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for PPARA drug discovery. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen & Mutants | PPARA LBD & Full-Length Recombinant Protein (Human/Mouse/Cyno). Including wild-type and key missense variants (dbSNP rs1800204, rs1800206, rs1800234). High purity (>95%), Endotoxin <1 EU/µg. Sequence Verified. Theoretical MW confirmed by Mass Spec. HEK293 expressed for native folding. | View PPARA Products |
| Gene Delivery | PPARA Premade Lentivirus Particles (Promise-ORF). Full-length ORF for stable reporter cell line construction. CMV promoter, Puromycin selection. | View PPARA Products |
| Selectivity Panel | PPAR Subfamily Panel (PPARA / PPARG / PPARD). Recombinant LBD proteins for counter-screening. Sequence verified, >95% purity. | View PPARA Products |
| Benchmark Ab | Anti-PPARA Recombinant Antibody. Positive control for western blot, target engagement, ChIP, IP, and expression validation. | View PPARA Products |
| Validator | PPARA siRNA Set (3 unique sequences). For knockdown verification and assay specificity control in cell-based assays. | View PPARA Products |
| Heterodimer Partner | RXRA Protein (human recombinant). Essential co-assembly partner for PPARA functional assays (co-activator recruitment, DNA binding). | View RXRA Products |
| Related Target A | PPARG LBD Protein. Critical for selectivity profiling and off-target liability assessment. | View PPARG Products |
| Related Target B | PPARD LBD Protein. For dual-agonist profiling and subfamily specificity validation. | View PPARD Products |
| Mutant Controls | PPARA LBD mutant panel (e.g., V318M, I352S corresponding to key variants). Used as negative controls for binding selectivity and resistance mechanism studies. | View PPARA Products |
Critical Assay Challenges & TarMart Solutions
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| Subfamily Counter-Screening (PPARα vs γ vs δ) | PPAR Pan-Panel: Human PPARA, PPARG, PPARD LBD proteins with >95% purity, sequence verified for binding assay standardization. |
| Co-activator Recruitment Assay (TR-FRET / AlphaScreen) | High-purity PPARA LBD with validated refolding protocol, preserving native conformation for coregulator interaction. |
| Cross-Species Preclinical Translation | Ortholog proteins available for Human, Cynomolgus, Mouse, and Rat PPARA LBD (sequence identity >95%). |
| Compound Specificity Validation in Cells | PPARA siRNA set included for target-specific signal confirmation; benchmark antibody for orthogonal engagement. |
| Nuclear Translocation / Reporter Assays | Full-length PPARA lentivirus particles for stable cell line generation (HEK293 expressed, native folding). |
| False Positive Control in Binding Assays | Mutant PPARA LBD constructs (ligand-binding pocket residues) offered as negative controls for probe selectivity. |
Live PPARA R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
- ➤ View Active Clinical Trials
- ➤ Latest Resistance & Selectivity Research
- ➤ Recent Patent Filings (SPPARMs & Modulators)
Global Clinical Landscape & Future Outlook
The PPARA therapeutic landscape is undergoing a strategic shift from broad-spectrum fibrates to next-generation Selective PPAR Alpha Modulators (SPPARMs). With pemafibrate (K-877) establishing proof-of-concept for improved lipid profiles without PPARγ-associated fluid retention, the race is intensifying for candidates with enhanced selectivity profiles for NASH and cardiovascular indications. As first-generation SPPARMs advance through Phase II/III, the next wave of R&D is targeting tissue-specific activation (liver-preferential), combination therapies with incretin pathways, and novel oncology indications where lipid metabolism reprogramming drives tumor survival. Additionally, early-stage PROTAC degraders are emerging for PPARA-driven malignancies, requiring degradation and ubiquitination assays. The integration of resistance mutation studies (e.g., rs1800204, rs1800206, rs1800234) is becoming standard for chronic treatment scenarios.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Small Molecule SPPARM | Kowa, Eli Lilly, Genfit | Dyslipidemia, NASH | Subfamily Selectivity Panel (PPARα/γ/δ) for liability screening |
| Pemafibrate Analogs | Kowa Research Institute | Hypertriglyceridemia | Human/Cyno PPARA LBD for cross-species potency correlation |
| Dual PPAR Agonists (α/γ or α/δ) | Inventiva, Genfit | NASH, Primary Biliary Cholangitis | Binding Affinity & Coregulator Assay (functionally folded native proteins) |
| Pan-PPAR Agonist | Inventiva | Metabolic Syndrome | Subfamily specificity profiling (full PPAR isoform protein trio) |
| PROTACs / Degraders | Early Stage Biotechs | Advanced Solid Tumors | Degradation & Ubiquitination Assays (HEK293 expressed targets & stable cell lines) |
| Gene Therapy (Preclinical) | Academic Labs | Rare Metabolic Disorders | High-titer PPARA lentivirus for stable expression studies |
Note: PPARA is an intracellular nuclear receptor. Therapeutic development focuses on small molecule modulators requiring high-precision protein-protein interaction assays. TarMart provides purified recombinant LBD proteins, subfamily panels, mutant controls, and ortholog reagents for accurate selectivity determination and preclinical translation.
Key Functional Domains & Genetic Variants
PPARA (UniProt Q07869) contains a Nuclear Receptor Ligand-Binding Domain (NR LBD) essential for ligand recognition and co-regulator recruitment. Clinically relevant missense variants include dbSNP rs1800204 (V318M), rs1800206 (I352S), and rs1800234 (L162V). These mutations affect ligand binding affinity and transactivation efficiency, making them critical for designing mutant protein controls, understanding patient stratification, and developing resistance-proof therapeutics. TarMart offers a panel of PPARA LBD mutants corresponding to these variants for selectivity and resistance mechanism studies.