Market Intelligence, Clinical Progress, and High-Purity Reagents for Osteoporosis, Hypoparathyroidism, and Calcium Homeostasis Development.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for PTH1R drug discovery. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Gene Delivery | PTH1R Lentivirus Premade Particles Full-length human PTH1R (NM_000316) with eGFP reporter. High Titer (>10^8 TU/mL). For stable cell line generation preserving native Class B GPCR conformation. |
View PTH1R Products |
| Antigen | PTH1R ECD-Fc Fusion Protein Extracellular domain (Met1-Gln188) fused to human IgG1 Fc. HEK293 expressed. Sequence Verified. High Purity (>95%). For binding and kinetic assays. |
View PTH1R Products |
| Ligand Control | Human PTH (1-84) Recombinant Protein Full-length native sequence. Bioanalytical grade for functional assays. |
View PTH Products |
| Ligand Control | Human PTHrP (1-141) Recombinant Protein High purity ligand for receptor activation studies. |
View PTHrP Products |
| Validator | PTH1R siRNA Set For knockdown verification. |
View PTH1R Products |
| Benchmark Ab | Anti-PTH1R Reference Antibody Recombinant positive control for flow cytometry and binding validation. |
View PTH1R Products |
| Related Target | CASR (Calcium-Sensing Receptor) Critical calcium homeostasis partner; essential for combination therapy screening and pathway analysis. |
View CASR Products |
| Selectivity Panel | PTH2R (Parathyroid Hormone 2 Receptor) Close homolog for counter-screening to ensure ligand specificity. |
View PTH2R Products |
Critical Assay Challenges & TarMart Advantages
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| Native GPCR Conformation (Class B structure with large ECD) | Lentivirus-mediated stable cell lines in HEK293 background; preserves post-translational modifications and 7TM topology for accurate ligand binding. |
| Gs/cAMP Pathway Activation Measurement | High-expression PTH1R cell lines enabling robust cAMP accumulation assays with low basal noise. |
| Cross-species Toxicology Evaluation (Cyno/Mouse/Rat) | Human/Mouse/Cyno/Rat ortholog lentivirus particles available with sequence-verified ORFs. |
| Internalization for ADC Development | High-expression stable lines compatible with pH-sensitive dye internalization assays; ECD-Fc available for binding affinity confirmation. |
| PTH1R vs PTH2R Selectivity | Strictly sequence-verified PTH2R counter-screening proteins by mass spec to eliminate off-target risks. |
| Lack of Positive Controls | Recombinant human PTH(1-84) and PTHrP ligands included for functional validation. |
| False Positives from Non-specific Signals | Validated siRNA included for specificity checks. |
Live PTH1R R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Global Clinical Landscape & Future Outlook
The race for PTH1R therapeutics is intensifying, with major players shifting focus from traditional daily PTH injections to long-acting peptide formulations, orally bioavailable small molecules, and targeted ADCs. As first-generation replacement therapies (TransCon PTH, Yorvipath) reach the clinic, the next wave of R&D is targeting biased agonism to uncouple bone formation from bone resorption, aiming to maximize anabolic effects while minimizing hypercalcemia risks. Additionally, tissue-selective signaling (bone vs. kidney) and novel modalities such as negative allosteric modulators (NAMs) for hyperparathyroidism inhibition are key frontiers. Key mutations including constitutively activating variants (e.g., in Jansen metaphyseal chondrodysplasia, JMC) drive the need for mutant-specific inverse agonists.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Peptide Analogs (Short- & Long-Acting) | Eli Lilly (Teriparatide), Radius Health (Abaloparatide), Ascendis Pharma (TransCon PTH) | Osteoporosis, Hypoparathyroidism | Receptor Binding & cAMP Assay (Need stable cell lines via Lentivirus) |
| Small Molecule Agonists | Chugai, EnteraBio (EB613) | Osteoporosis, Hypoparathyroidism | cAMP/Calcium Flux (Require high-expression GPCR cell lines) |
| Negative Allosteric Modulators (NAMs) | BridgeBio (Encaleret) | Autosomal Dominant Hypocalcemia Type 1 (ADH1) | Binding Affinity & Selectivity (Need human/mutant PTH1R proteins) |
| Monoclonal Antibodies | Various Biotechs | Rare Bone Diseases | Epitope Mapping (Need high-purity ECD-Fc proteins) |
| Antibody-Drug Conjugates (ADCs) | Molecular Templates (MT-1911) | Secondary Hyperparathyroidism (CKD) | Internalization Assay (Need high-expression lentivirus stable lines) |
| Oral PTH | EnteraBio (EB613) | Osteoporosis | Receptor Internalization & Recycling Kinetics |
Related Targets for Integrated Research
Explore complementary targets to build a comprehensive assay panel:
- PTH (Parathyroid Hormone): Endogenous ligand for signaling validation.
- PTHrP (Parathyroid Hormone-related Protein): Key in humoral hypercalcemia of malignancy; recombinant protein available.
- CASR (Calcium-Sensing Receptor): Central partner in calcium homeostasis; combination therapy screening.
- PTH2R (Parathyroid Hormone 2 Receptor): Close homolog for selectivity counter-screening.
- RANKL / RANK: Downstream nodes in bone remodeling, crucial for assessing osteoblast-osteoclast crosstalk.
Key Mutations & Variants for Functional Studies
Understanding the impact of PTH1R mutations is critical for developing targeted therapies:
- Constitutively activating mutation (MCDJ/JMC): dbSNP:rs121434599 (Val223Arg?) Actually fact_payload lists “in MCDJ; constitutively activates adenylate cyclase-ac”. UniProt VAR_003582. This mutant is used to screen inverse agonists.
- Other naturally occurring variants: dbSNP:rs121434599 (BOCD) and rs121434601 (BOCD). These may affect ligand binding or signaling.
TarMart offers customized mutant protein and lentivirus particles for these variants upon request.