Powder: -20°C for 3 years | In solvent: -80°C for 2 years
NPS-2143 is a novel potent and selective antagonist of Ca(2+) receptor.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
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 )
You can also refer to dose conversion for different animals. More
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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