Name | NPS-2143 hydrochloride |
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Synonyms |
MFCD16038896
Benzonitrile, 2-chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino]-2-hydroxypropoxy]-, hydrochloride (1:1) 2-Chloro-6-[(2R)-2-hydroxy-3-{[2-methyl-1-(2-naphthyl)-2-propanyl]amino}propoxy]benzonitrile hydrochloride (1:1) NPS-2143 (hydrochloride) |
Description | NPS-2143(SB 262470A ) 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.IC50 value: 43 nM(for Ca2+ receptor) [1]Target: CaSRin 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 [1]. 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 [2].in vivo: When infused intravenously in normal rats, NPS 2143 caused a rapid and large increase in plasma levels of PTH. Ca2+ receptor antagonists are termed calcilytics and NPS 2143 is the first substance (either atomic or molecular) shown to possess such activity [1]. When administered together with an antiresorptive agent (estradiol), NPS 2143 causes an increase in trabecular bone volume and bone mineral density in osteopenic rats [2]. |
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Related Catalog | |
References |
Molecular Formula | C24H26Cl2N2O2 |
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Molecular Weight | 445.381 |
Exact Mass | 444.137146 |
Storage condition | 2-8°C |
Symbol |
GHS07, GHS09 |
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Signal Word | Warning |
Hazard Statements | H302 + H312 + H332-H410 |
Precautionary Statements | P273-P280-P501 |
Hazard Codes | Xn,N |
Risk Phrases | 20/21/22-50/53 |
Safety Phrases | 36/37-60-61 |
RIDADR | UN 3077 9 / PGIII |