| Name | NPS-2143 hydrochloride |
| Description | NPS-2143 hydrochloride (NPS-2143 HCL) is a selective potent calcium ion-sensing receptor antagonist. |
| In vitro | NPS 2143, even when tested at much higher concentrations (3 microM), did not affect the activity of a number of other G protein-coupled receptors, including those most structurally homologous to the Ca2+ receptor. NPS 2143 stimulated parathyroid hormone (PTH) secretion from bovine parathyroid cells (EC50 of 41 nM) over a range of extracellular Ca2+ concentrations and reversed the effects of the calcimimetic compound NPS R-467 on [Ca2+]i and on secretion of PTH . The first reported calcilytic compound was NPS 2143, an orally active molecule which elicits rapid, 3- to 4-fold increases in circulating levels of PTH. |
| In vivo | When intravenously administered to normal rats, NPS 2143 swiftly elevated plasma PTH levels significantly. Known as calcilytics, substances like NPS 2143 act as Ca2+ receptor antagonists, with it being the inaugural compound (either atomic or molecular) identified with this activity [1]. Concurrent administration with an antiresorptive agent (estradiol) resulted in enhanced trabecular bone volume and bone mineral density in osteopenic rats. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (112.26 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.49 mM), Sonication is recommended.
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| Keywords | SB-262470A | NPS-2143 Hydrochloride | NPS2143 hydrochloride | NPS2143 Hydrochloride | NPS-2143 | NPS2143 | NPS 2143 Hydrochloride | NPS 2143 hydrochloride | NPS 2143 | Inhibitor | inhibit | CaSR | Calcium-sensing receptor |
| Inhibitors Related | SB-423562 | Strontium ranelate | Cinacalcet | Tecalcet Hydrochloride | NPS-2143 | Strontium chloride | Calindol hydrochloride | Poly-D-lysine hydrobromide (MW 30000-70000) | Cinacalcet hydrochloride | AC265347 | Evocalcet | Gadolinium chloride |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Preclinical Compound Library | GPCR Compound Library | Anti-Metabolism Disease Compound Library | Anti-COVID-19 Compound Library |
United States
