NPS 2143 Inhibitor CAS No. 284035-33-2

Cat. No.	Name	Size	Price
KI1135	NPS 2143	10 mg	$192
	NPS 2143	50 mg	$752
	NPS 2143	200 mg	$2032

Chemical Characteristic

Product Name	NPS 2143
CAS No.	284035-33-2
Molecular Weight	408.92
Formula	C₂₄H₂₅ClN₂O₂
Chemical Name	2-chloro-6-[(2R)-2-hydroxy-3-[(2-methyl-1-naphthalen-2-ylpropan-2-yl)amino]propoxy]benzonitrile
Smiles	C(#N)c1c(cccc1OC[C@@H](CNC(Cc1cc2c(cc1)cccc2)(C)C)O)Cl
Chemical Structure

Biological activities

NPS 2143 is a novel, selective antagonist of the parathyroid cell Ca²⁺ receptor. NPS 2143 inhibits extracellular Ca²⁺-evoked increases in [Ca²⁺]_{i in HEK 293 cells with an IC50 of 43 nM. NPS 2143 stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells in vitro with an EC50 of 41 nM. ^[1] NPS 2143 reverses the effects of the calcimimetic compound NPS R-467 on [Ca²⁺]_{i and on secretion of PTH. NPS 2143 augments the amount of PTH appearing in the medium during a 20-minute incubation. NPS 2143 augments cyclic AMP levels at low concentrations of extracellular Ca²⁺ and completely blocks the inhibitory effects of 2 mM extracellular Ca²⁺ on evoked increased in cyclic AMP levels. ^[2] NPS-2143 diminishes the responsiveness to [Ca²⁺]_{o in the CaSR mutants T151R, E767Q, G830S, and A844T. ^[3] Administered together with an antiresorptive agent (estradiol), NPS 2143 causes an increase in trabecular bone volume and bone mineral density in osteopenic rats. ^[1]}}}

Protocols

NPS 2143 is dissolved in DMSO, and used at final concentrations of 1 µM and 300 nM with DMSO at 0.1%. ^[3]

References

[1] Nemeth EF, et al. The search for calcium receptor antagonists (calcilytics). J Mol Endocrinol. 2002, 29(1): 15-21. [2] Nemeth EF, et al. Calcilytic compounds: potent and selective Ca²⁺ receptor antagonists that stimulate secretion of parathyroid hormone. J Pharmacol Exp Ther. 2001, 299(1): 323-331. [3] Letz S, et al. Novel activating mutations of the calcium-sensing receptor: the calcilytic NPS-2143 mitigates excessive signal transduction of mutant receptors. J Clin Endocrinol Metab. 2010, 95(10): E229-E233

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