Catalog No.S2633 Synonyms: SB262470
Molecular Weight(MW): 408.92
NPS-2143 is a novel potent and selective antagonist of Ca(2+) receptor with IC50 of 43 nM.
1 Customer Review
The effects of a GPRC6A inhibitor on testosterone-induced ROS generation. Cells were pretreated with the GPRC6A inhibitor, NPS2143 (1 uM), for 30 min and ROS generation was monitored after 5 min of testosterone treatment. Data are presented as mean ?S.E. (n = 4).
J Biol Chem 2014 289(42), 28835-45. NPS-2143 purchased from Selleck.
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|Description||NPS-2143 is a novel potent and selective antagonist of Ca(2+) receptor with IC50 of 43 nM.|
NPS 2143 blocks increases in cytoplasmic Ca2+ concentrations with IC50 of 43 nM elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor.  NPS 2143 stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells with EC50 of 41 nM. Moreover, NPS 214 also blocks the inhibitory effects of calcimimetic NPS R-467 on PTH secretion from bovine parathyroid cells and the inhibitory effects of extracellular Ca2+ on isoproterenol-stimulated increases in cyclic AMP formation.  In HEK-293 cells transiently expressing hCaSRs, NPS 2143 significantly suppresses the kokumi taste by effectively inhibiting the activity of both GSH (data not shown) and γ-Glu-Val-Gly.  A recent study shows that NPS 2143 treatment suppresses low molecular weight fractions of azuki hydrolysate-induced cholecystokinin (CCK) secretion in CaSR-transfected HEK 293 cells. 
|In vivo||In rats, NPS 2143 results in a rapid 4- to 5-fold increase in plasma PTH levels and also a transient increase in plasma Ca2+ levels.  In normotensive rats, NPS 2143 administration (1 mg/kg) by i.v. markedly increases mean arterial blood pressure (MAP) in the presence of parathyroid glands. |
|In vitro||DMSO||82 mg/mL (200.52 mM)|
|In vivo||2% DMSO+corn oil||10mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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