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Catalog No.
CaSR antagonist
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NPS-2143 is a novel and selective antagonist of CaSR (Ca2+-sensing receptor) with the EC50 value of 4.27mM for [Ca2+]o [1].

Calcilytics NPS-2143 has been reported to diminish the sensitivity of the CaSR for [Ca2+]o, resulting in an attenuated signal transduction in vitro and increased secretion of PTH in vivo. In addition, The EC50 values of NPS-2143 are 4.27, 1.56, 1.61, 2.46, 2.07 and 3.15mM for the wild-type CaSR, mutant CaSR (T151R, P221L, E767Q, G830S, and A844T), respectively. Apart from these, in HEK 293T cells expressing CaSR, NPS-2143 has been revealed to inhibit the [Ca2+]o-induced cytosolic calcium signal in a concentration-dependent manner [1].

[1] Letz S1, Rus R, Haag C, Dörr HG, Schnabel D, Möhlig M, Schulze E, Frank-Raue K, Raue F, Mayr B, Schöfl C. Novel activating mutations of the calcium-sensing receptor: the calcilytic NPS-2143 mitigates excessive signal transduction of mutant receptors. J Clin Endocrinol Metab. 2010 Oct;95(10):E229-33.


Chemical Properties

StorageStore at -20°C
Cas No.284035-33-2
Solubility≥40.9 mg/mL in DMSO; insoluble in H2O; ≥28.35 mg/mL in EtOH
Chemical Name2-chloro-6-[(2R)-2-hydroxy-3-[(2-methyl-1-naphthalen-2-ylpropan-2-yl)amino]propoxy]benzonitrile
SDFDownload SDF
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description NPS-2143 is a novel potent and selective antagonist of Ca(2+) receptor with IC50 of 43 nM.
Targets Ca(2+) receptor          
IC50 43 nM          

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