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NPS-2143

Catalog No. T1730 CAS 284035-33-2

Synonyms: SB 262470A, NPS 2143, SB262470

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

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NPS-2143, CAS 284035-33-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 79.00
25 mg	In stock	$ 156.00
50 mg	In stock	$ 232.00
100 mg	In stock	$ 347.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 98.24%

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Description	NPS-2143 is a novel potent and selective antagonist of Ca(2+) receptor.
Targets&IC50	Ca(2+) receptor:43 nM
Kinase Assay	This clonal cell line, referred to as HEK 293 4.0-7 cells, are used in a high-throughput screening format to detect agonists and allosteric activators of the Ca2+?receptor. Changes in the concentration of cytoplasmic [Ca2+]i provide a quantitative and functional assessment of Ca2+ receptor activity in these cells and the results using this assay parallel those obtained using a homologous expression system of bovine parathyroid cells. On-line continuous measurements of fluorescence in fluo-3- or fura-2-loaded HEK 293 4.0-7 cells are obtained using a custom-built spectrofluorimeter or a fluorescence imaging plate reader instrument. NPS-2143 is incubated with cells for 1 minute before increasing the concentration of extracellular Ca2+?from 1.0 mM to 1.75 mM. NPS-2143 is tested individually at a concentration of 100 μg/mL (20 μM-80 μM) and those causing more than a 40% inhibition of the control response are considered to be biologically active. To determine the potencies (IC50) of NPS-2143 with biological activity, concentration-response curves are obtained and then, as an initial assessment of selectivity, the effects of NPS-2143 on [Ca2+]i evoked by other G protein-coupled receptors are examined at a concentration several times their IC50. Wild-type HEK 293 cells (and HEK 293 4.0-7 cells) express receptors for thrombin, bradykinin, and ATP, which couple to the mobilization of intracellular Ca2+. These responses can be studied to quickly assess any nonselective action of compounds on G protein-coupled receptors. Additional assays for selectivity include HEK 293 cells engineered to express receptors most homologous in sequence and topology to the Ca2+ receptor. These include native or chimeric receptors for various metabotropic glutamate and γ-aminobutyric acid type B receptors (GABABRs).Chimeric receptors are created using partial sequences of metabotropic glutamate receptors and Ca2+?receptors, engineered to couple to activation of phospholipase C and release of intracellular Ca2+?in HEK 293 cells. NPS-2143 lacking pan-activity are then subjected to structural modifications and their potencies and selectivities monitored using these HEK 293 4.0-7 cell assays in an iterative process.

Synonyms	SB 262470A, NPS 2143, SB262470
Molecular Weight	408.92
Formula	C24H25ClN2O2
CAS No.	284035-33-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

Ethanol: <1 mg/mL

H2O: <1 mg/mL

DMSO: ＜1 mg/mL (2.45 mM）, Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Nemeth EF, et al. J Pharmacol Exp Ther. 2001, 299(1), 323-331. 2. Rybczynska A, et al. J Endocrinol. 2006, 191(1), 189-195. 3. Ohsu T, et al. J Biol Chem. 2010, 285(2), 12016-1022. 4. Nakajima S, et al. Mol Nutr Food Res. 2012, 56(5), 753-760.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Anti-Obesity Compound Library ReFRAME Related Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Orally Active Compound Library Ion Channel Inhibitor Library Anti-Cardiovascular Disease Compound Library Bioactive Compound Library Preclinical Compound Library

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Keywords

NPS-2143 284035-33-2 GPCR/G Protein Membrane transporter/Ion channel Metabolism CaSR Calcium Channel SB-262470A Inhibitor NPS2143 SB 262470A inhibit NPS 2143 Calcium-sensing receptor SB262470 inhibitor

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