NR1D1 (Nuclear Receptor Subfamily 1 Group D Member 1, commonly known as Rev-Erb alpha) is a ligand-sensitive transcription factor that acts as a primary coordinator of the mammalian circadian clock, metabolic pathways, and inflammatory responses. As an intracellular nuclear receptor, NR1D1 has emerged as a high-value therapeutic target for metabolic syndrome, non-alcoholic steatohepatitis (NASH), sleep disorders, and specific oncology indications where circadian disruption drives disease progression.
TarMart Solution Ecosystem & Related Targets
TarMart provides high-specification reagents designed to support target validation, binding assays, and cell-based screening for NR1D1 drug discovery programs. Select your product modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen | NR1D1 Recombinant LBD / DBD Protein High purity (>95%), Sequence Verified, Theoretical MW confirmed. Suitable for biophysical binding assays. |
View NR1D1 Products |
| Gene Delivery | NR1D1 Lentivirus / Expression Plasmid Full-length ORF sequence for stable cell line generation and reporter gene assays. |
View NR1D1 Products |
| Benchmark Ab | Anti-NR1D1 Recombinant Antibody Sequence-verified positive control for Western Blot, IHC, and IP validation. |
View NR1D1 Products |
| Validator | NR1D1 siRNA Set Target-specific knockdown pool for functional specificity verification. |
View NR1D1 Products |
| Related Target A | NR1D2 (Rev-Erb beta) Subfamily homolog; critical for selectivity profiling and dual-agonist development. |
View NR1D2 Products |
| Related Target B | ARNTL (BMAL1) Direct downstream transcriptional target of NR1D1; essential for pathway readout assays. |
View ARNTL Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| Selectivity profiling against homolog NR1D2 | Human NR1D1 and NR1D2 recombinant proteins strictly verified by mass spectrometry for sequence accuracy. |
| Intracellular localization & cellular assay setup | High-titer Lentivirus particles ready for stable cell line construction to run reporter gene assays. |
| Lack of verified controls | Recombinant positive control antibodies and sequence-verified siRNA pools included in the catalog. |
| Assay noise from bacterial endotoxins | Endotoxin-controlled expression systems ensuring <1 EU/ug for cell-based validation. |
Live NR1D1 R&D Tracker
The global pipeline for circadian-related nuclear receptors is evolving rapidly. Monitor real-time academic and clinical developments using these direct search trackers:
Global Clinical Landscape & Future Outlook
Therapeutics targeting NR1D1 are predominantly focused on small molecule modulation. Since NR1D1 naturally binds heme to repress transcription, drug discovery efforts are heavily oriented toward synthetic agonists (such as SR9009 and SR9011 derivatives) and selective antagonists. The field is actively shifting from systemic, broad-spectrum agonists—which often present pharmacokinetic challenges—to tissue-targeted molecules and dual NR1D1/NR1D2 modulators. This evolution is designed to optimize circadian phase-shifting capabilities without triggering off-target metabolic toxicity.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Small Molecule Agonist | Ryvu Therapeutics, Academic Spin-offs | Solid Tumors (Glioblastoma, Breast), NASH | High-purity LBD protein for SPR/TR-FRET ligand binding assays. |
| Dual NR1D1/2 Modulators | Salk Institute, Clinical Stage Biotechs | Circadian Rhythm Disorders, Metabolic Syndrome | Cross-reactivity panels (NR1D1 vs NR1D2 recombinant proteins). |
| Gene Regulation / RNAi | Preclinical Research Labs | Inflammatory Diseases, Cardiovascular Disease | Sequence-verified siRNA and Lentivirus for target knockdown and rescue assays. |