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NPS-2143 (SB262470) is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively. NPS-2143 blocks increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells . NPS-2143 (SB262470), even at much higher concentrations (3 μM), did not influence the activity of a number of other G protein-coupled receptors, including those most structurally homologous to the Ca2+ receptor.NPS-2143 (SB262470) also stimulates parathyroid hormone secretion from bovine parathyroid cells . In addition, administration of NPS-2143 resulted in moderate but sustained increases in plasma PTH levels and marked increases in bone formation and resorption with no net bone gain or loss.
Advanced Fiber Materials. 2024 Jul 01.
Remodeling Electrophysiological Microenvironment for Promoting Bone Defect Repair via Electret Hybrid Electrospun Fibrous Mat
NPS-2143 purchased from AbMole
CEJ. 2020 Dec;Volume 402, 126203.
Periosteum structure/function-mimicking bioactive scaffolds with piezoelectric/chem/nano signals for critical-sized bone regeneration
NPS-2143 purchased from AbMole
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Source | Chemical Engineering Journal (2020 Dec). Figure 5. NPS2143 (Abmole Bioscience, US) |
| Method | Mechanism analysis | |
| Cell Lines | BMSCs | |
| Concentrations | 10 mM | |
| Incubation Time | 24 h | |
| Results | Furthermore, CaSR blocking assays were performed to evaluate the effect of CaSR on osteogenic differentiation by adding NPS2143 in unp-PVFT and p-PVFT (unp-PVFT-AntiCaSR and p-PVFT-AntiCaSR) |
| Cell Experiment | |
|---|---|
| Cell lines | HEK 293 4.0-7 cells |
| Preparation method | On-line continuous measurements of fluorescence in fluo-3- or fura-2-loaded HEK 293 4.0-7 cells are obtained using a custom-built spectrofluorimeter or a fluorescence imaging plate reader instrument. NPS-2143 is incubated with cells for 1 minute before increasing the concentration of extracellular Ca2+ from 1.0 mM to 1.75 mM. NPS-2143 is tested individually at a concentration of 100 μg/mL (20 μM-80 μM) and those causing more than a 40% inhibition of the control response are considered to be biologically active. |
| Concentrations | 20 μM-80 μM |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Chronic indwelling catheters are implanted in the inferior vena cava and in the abdominal aorta of male Sprague-Dawley rats. |
| Formulation | NPS 2143 is dissolved in 20% aqueous solution of 2-hydroxypropyl-β-cyclodextrin. |
| Dosages | ≤0.1 μmol/kg · min |
| Administration | Administered via i.v. |
| Molecular Weight | 408.92 |
| Formula | C24H25ClN2O2 |
| CAS Number | 284035-33-2 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Calcium-sensing Receptor Products |
|---|
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Strontium ranelate, a therapeutic for osteoporosis, was thought to have a dual mode of action, simultaneously stimulating bone formation and reducing resorption. |
| Ligustroflavone
Ligustroflavone, which can be extracted from Ligustrum lucidum, is a potential calcium sensitive receptor (CaSR) antagonist. Ligustroflavone has protective effect on diabetic osteoporosis mice. |
| Cinacalcet
Cinacalcet(AMG-073) is an orally active, second-generation calcimimetic compound; AMG 073 represents a new class of compounds for the treatment of hyperparathyroidism. |
| Cinacalcet HCl
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| Calcium-Sensing Receptor Antagonists I
Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors. |
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