Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NPS-2143 hydrochloride (NPS-2143 HCL) is a selective potent calcium ion-sensing receptor antagonist.
説明 | NPS-2143 hydrochloride (NPS-2143 HCL) is a selective potent calcium ion-sensing receptor antagonist. |
ターゲット&IC50 | CaSR:43nM/41nM |
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. |
別名 | NPS-2143 HCL |
分子量 | 445.38 |
分子式 | C24H25ClN2O2.HCl |
CAS No. | 324523-20-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (112.26 mM)
You can also refer to dose conversion for different animals. 詳細
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NPS-2143 hydrochloride 324523-20-8 GPCR/G Protein CaSR NPS2143 NPS 2143 Hydrochloride NPS2143 Hydrochloride NPS-2143 NPS 2143 hydrochloride Calcium-sensing receptor inhibit SB-262470A Inhibitor NPS-2143 Hydrochloride NPS 2143 NPS-2143 HCL NPS2143 hydrochloride inhibitor