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NPS-2143 CaSR antagonist

Name: NPS-2143
Brand: Selleck Chemicals
SKU: S2633
Availability: InStock
Rating: 5 (21 reviews)

Cat.No.S2633

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

Chemical Structure

Molecular Weight: 408.92

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.72%

99.72

Related Targets	Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras GPR GluR Prostaglandin Receptor CXCR Adenosine Receptor P2 Receptor CCR Angiotensin Receptor Hedgehog/Smoothened S1P Receptor PKA Cannabinoid Receptor cAMP Glucagon Receptor SGLT Opioid Receptor Sigma Receptor PAR Endothelin Receptor LTR Neurokinin Receptor Guanylate Cyclase PKG LPA Receptor

Chemical Information, Storage & Stability

Molecular Weight	408.92	Formula	C₂₄H₂₅ClN₂O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	284035-33-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SB262470			Smiles	CC(C)(CC1=CC2=CC=CC=C2C=C1)NCC(COC3=C(C(=CC=C3)Cl)C#N)O

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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]
References	https://pubmed.ncbi.nlm.nih.gov/11561095/ https://pubmed.ncbi.nlm.nih.gov/17065402/ https://pubmed.ncbi.nlm.nih.gov/19892707/ https://pubmed.ncbi.nlm.nih.gov/22648622/

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