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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 |
|---|
| Encaleret
Encaleret is an orally active calcium-sensitive receptor (CaSR) antagonist for studies related to osteoporosis and autosomal dominant hypocalcemia (ADH1). |
| SB-423562
SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist. SB-423562 has the potential for osteoporosis research. |
| SB-423557
SB-423557 is an orally active calcium-sensing receptor (CaR) antagonist (IC50=520 nM), precursor of SB-423562 (IC50=73 nM). SB-423557 is well tolerated in human and increases plasma concentrations of exogenous parathyroid hormone (PTH) and stimulates bone formation. |
| Etelcalcetide
Etelcalcetide (AMG 416) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis. |
| Upacicalcet
Upacicalcet is a calcium-sensing receptor (CaSR) agonist being developed for the study of secondary hyperparathyroidism (SHPT). |
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