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NPS-2143 CaSR antagonist

Catalog No.B1424
Size Price Stock Qty
5mg
$60.00
In stock
10mg
$85.00
In stock
50mg
$320.00
In stock
200mg
$930.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

NPS-2143

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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Chemical Properties

Cas No. 284035-33-2 SDF Download SDF
Chemical Name 2-chloro-6-[(2R)-2-hydroxy-3-[(2-methyl-1-naphthalen-2-ylpropan-2-yl)amino]propoxy]benzonitrile
Canonical SMILES CC(C)(CC1=CC2=CC=CC=C2C=C1)NCC(COC3=C(C(=CC=C3)Cl)C#N)O
Formula C24H25ClN2O2 M.Wt 408.93
Solubility ≥40.9mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

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].

References:
[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.

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