Market Intelligence, Clinical Progress, and High-Purity Reagents for Autoimmune and Oncology Development
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for C5AR1 drug discovery. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen / Extracellular Domain | C5AR1 N-terminal ECD-Fc Fusion Protein. High purity (>95%), Endotoxin <1EU/µg. HEK293 expressed with native glycosylation. Sequence verified. | View C5AR1 Products |
| Lentiviral Expression | C5AR1 Full-Length ORF Lentivirus. Codon-optimized for mammalian expression, CMV promoter. High titer (>10^8 TU/mL) for stable GPCR cell line generation. Preserves multi-pass native conformation. | View C5AR1 Products |
| Ligand Control | C5a (Complement C5a) Recombinant Protein. High purity (>95%), Sequence Verified, Endotoxin <1EU/µg. For competitive binding studies. | View C5a Products |
| Benchmark Antibody | Anti-C5AR1 Reference Monoclonal Antibody (Sequence of Avdoralimab). Recombinant positive control for flow cytometry and assay benchmarking. | View C5AR1 Products |
| Gene Silencing | C5AR1 siRNA Set (3 unique sequences). For knockdown validation and specificity controls. | View C5AR1 Products |
| Related Target A: C5 | Complement C5 Protein. Precursor to C5a; upstream pathway component for combination studies. | View C5 Products |
| Related Target B: C5AR2 | C5L2 (C5aR2) Lentivirus & Protein. Decoy receptor; critical for selectivity counter-screening assays. | View C5AR2 Products |
| Related Target C: C3AR1 | C3a Receptor (C3AR1) Reagents. Synergistic complement pathway target for dual-receptor profiling. | View C3AR1 Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| GPCR Conformation Integrity & Membrane Insertion | Lentiviral delivery ensures native folding, glycosylation, and membrane topology in stable cell lines. |
| C5AR1 vs C5AR2 (C5L2) Selectivity Screening | Homolog receptor panel (C5AR1, C5AR2) available, sequence verified for precise selectivity screening. |
| Species Cross-Reactivity (Cyno/Mouse/Human) | Human/Cyno/Mouse C5AR1 ortholog proteins available with Sequence Verified identity >95%. |
| Functional Calcium Flux Assay Setup | High-titer premade lentiviral particles for rapid generation of assay-ready cell lines (Calcium Flux ready). |
| Ligand Binding Validation | Recombinant C5a protein supplied with confirmed theoretical MW and purity for competitive binding studies. |
| Lack of Reliable Controls | Clinical Benchmark Antibodies (Biosimilars) included for assay standardization. |
Live C5AR1 (CD88) R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
- ➤ View Active Clinical Trials (C5aR / C5AR1 / CD88)
- ➤ Latest Resistance & Biased Signaling Research
- ➤ Recent Patent Filings
Global Clinical Landscape & Future Outlook
The C5aR therapeutic space entered a new era following the 2021 FDA approval of Avacopan (Tavneos), the first oral selective C5aR antagonist for ANCA-associated vasculitis. This validated the "C5a–C5aR" axis as a druggable target distinct from pan-complement inhibition (e.g., C5 blockade with Eculizumab). Current R&D trends show a strategic pivot from systemic complement inhibition to targeted receptor antagonism, with major efforts in:
- Immuno-Oncology: Tumor-associated macrophage (TAM) reprogramming via C5aR inhibition to enhance anti-PD-1 efficacy, focusing on the tumor microenvironment (TME).
- Acute Inflammation: Severe COVID-19 ARDS and sepsis modulation via rapid C5aR antagonism.
- Dermatology: Hidradenitis Suppurativa (HS) and psoriasis targeting the complement-inflammatory cascade.
- Neuroinflammation: Alzheimer’s disease and other chronic neuro-inflammatory disorders under preclinical investigation.
As first-generation small molecules establish safety profiles, the next wave focuses on biased signaling antagonists (β-arrestin sparing) to preserve immunoprotective functions while blocking pro-inflammatory signaling. The pipeline also increasingly features monoclonal antibodies and advanced modalities for TME immunosuppression.
Known Genetic Variants
Two polymorphisms in C5AR1 are documented in dbSNP:
- rs4467185 (UniProt VAR_049377)
- rs11880097 (UniProt VAR_049378)
These variants may influence receptor expression or function, though their clinical significance remains under investigation. Consideration of these variants is relevant for designing genotyping assays and understanding population-specific drug responses.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Small Molecule Antagonist | ChemoCentryx (Amgen), Takeda (Avacopan), Nodus Therapeutics (NDP-323) | ANCA Vasculitis, C3 Glomerulopathy | Calcium Flux Assay (Need stable C5AR1-expressing cell lines via Lentivirus) |
| Anti-C5aR Monoclonal Antibody | Innate Pharma (IPH5401-discontinued), Emerging biotechs | Solid Tumors, HS | Receptor Internalization Assay (Need high-purity ECD-Fc for binding) |
| Anti-C5a (Ligand-Targeted) | InflaRx (Vilobelimab), ChemoCentryx | Sepsis, COVID-19 | Ligand-Receptor Cross-Inhibition (Need recombinant C5a & C5AR1 pair) |
| Peptide Antagonists | Academic/Preclinical (PMX-53 derivatives) | Rheumatoid Arthritis | Competitive Binding Assay (Need N-terminal C5AR1 ECD) |
TarMart delivers the molecular tools to differentiate your C5aR program—whether pursuing orthosteric antagonism or allosteric modulation.