NPS-2143

Catalog No.S2633 Synonyms: SB262470

NPS-2143 Chemical Structure

Molecular Weight(MW): 408.92

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

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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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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 [1]
43 nM
In vitro

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. [1] 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. [1] 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. [3] 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. [4]

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. [1] 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. [2]

Protocol

Animal Research:[1]
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  • Animal Models: Chronic indwelling catheters are implanted in the inferior vena cava and in the abdominal aorta of male Sprague-Dawley rats.
  • Formulation: NPS 2143 is dissolved in 20% aqueous solution of 2-hydroxypropyl-β-cyclodextrin.
  • Dosages: ≤0.1 μmol/kg · min
  • Administration: Administered via i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 82 mg/mL (200.52 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+corn oil 10mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 408.92
Formula

C24H25ClN2O2

CAS No. 284035-33-2
Storage powder
in solvent
Synonyms SB262470

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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CaSR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID