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.
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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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| SB-423562
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| 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
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