Home GPCR & G Protein CaSR antagonist NPS-2143 For research use only.

NPS-2143

Synonyms: SB262470

NPS-2143 (SB262470) is a novel potent and selective antagonist of Ca(2+) receptor with IC50 of 43 nM.

NPS-2143 Chemical Structure

NPS-2143 Chemical Structure

CAS No. 284035-33-2

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NPS-2143 Related Products

Signaling Pathway

CaSR Signaling Pathways

CaSR Signaling Pathway

Biological Activity

Description NPS-2143 (SB262470) 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
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 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]
Animal Research Animal Models Chronic indwelling catheters are implanted in the inferior vena cava and in the abdominal aorta of male Sprague-Dawley rats.
Dosages ≤0.1 μmol/kg · min
Administration Administered via i.v.

Chemical Information & Solubility

Molecular Weight 408.92 Formula

C24H25ClN2O2
CAS No. 284035-33-2 SDF Download NPS-2143 SDF
Smiles CC(C)(CC1=CC2=CC=CC=C2C=C1)NCC(COC3=C(C(=CC=C3)Cl)C#N)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 82 mg/mL ( (200.52 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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