Home Tools

Cart

NPS-2143

Catalog No. T1730 CAS 284035-33-2

Synonyms: SB262470, NPS 2143, SB 262470A

NPS-2143 (SB 262470A) is a novel potent and selective antagonist of Ca(2+) receptor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

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 (in DMSO)	In stock	$ 52.00

Bulk Inquiry

Select Batch

Purity: 98.24%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	NPS-2143 (SB 262470A) is a novel potent and selective antagonist of Ca(2+) receptor.
Targets&IC50	Ca2+ receptor:43 nM
In vitro	NPS 2143 stimulates the secretion of parathyroid hormone (PTH) from bovine parathyroid cells with an effective concentration (EC50) of 41 nM. Moreover, NPS 2143 inhibits the suppressive effect of the calcimimetic NPS R-467 on PTH secretion from bovine parathyroid cells and the inhibition of cAMP formation stimulated by isoproterenol in the presence of extracellular Ca2+. In HEK 293 cells expressing the human Ca2+ receptor, NPS 2143 blocks the increase in cytosolic Ca2+ concentration induced by receptor activation, with an inhibitory concentration (IC50) of 43 nM. Furthermore, in HEK-293 cells transiently expressing hCaSRs, NPS 2143 significantly inhibits the umami taste perception by effectively suppressing GSH (data not shown) and γ-Glu-Val-Gly activity.
In vivo	In normotensive rats, intravenous administration of NPS 2143 (1 mg/kg) significantly increased mean arterial pressure (MAP) in the presence of the parathyroid gland. Additionally, NPS 2143 induced a rapid 4-5 fold increase in plasma parathyroid hormone (PTH) levels and an instantaneous rise in plasma calcium (Ca2+) levels.
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	SB262470, NPS 2143, SB 262470A
Molecular Weight	408.92
Formula	C24H25ClN2O2
CAS No.	284035-33-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: ＜1 mg/mL (2.45 mM）, Sonication is recommended.

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

Related Products

Related compounds with same targets

1-(aminomethyl)cyclopropanecarboxylic acid hydrochloride YM-244769 dihydrochloride Amlodipine Besylate 4-Hydroxycinnamamide Araloside X Caloxin 3A1 Butamben Dronedarone

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.