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NPS-2143

NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor[1][2].

Product Specifications

CAS Number

284035-33-2

Product Name Alternative

SB-262470A

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

CaSR

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/NPS-2143.html

Purity

99.94

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

N#CC1=C(OC[C@@H](CNC(C)(CC2=CC=C3C=CC=CC3=C2)C)O)C=CC=C1Cl

Molecular Formula

C24H25ClN2O2

Molecular Weight

408.92

Precautions

H315, H319, H320

References & Citations

[1]Nemeth EF, et al. Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone. J Pharmacol Exp Ther. 2001 Oct;299 (1) :323-31.|[2]Rybczynska A, et al. Hypertensive effect of calcilytic NPS 2143 administration in rats. J Endocrinol. 2006 Oct;191 (1) :189-95.|[3]Ohsu T, et al. Involvement of the calcium-sensing receptor in human taste perception. J Biol Chem. 2010 Jan 8;285 (2) :1016-22|[4]Nakajima S, et al. Calcium-sensing receptor mediates dietary peptide-induced CCK secretion in enteroendocrine STC-1 cells. Mol Nutr Food Res. 2012 May;56 (5) :753-60|[5]Sun J, et al. Calcium-sensing receptor: a sensor and mediator of ischemic preconditioning in the heart. Am J Physiol Heart Circ Physiol. 2010 Nov;299 (5) :H1309-17.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Citation 01

Acta Physiol. 2023 Apr;237 (4) :e13926.|Am J Physiol Heart Circ Physiol. 2010 Nov;299 (5) :H1309-17.|FEBS Open Bio. 2025 Oct 13.|Food Chem. 2024 Oct 10;464 (Pt 1) :141569.|Food Funct. 2022 Jun 6;13 (11) :6233-6243.|Food Funct. 2025 Apr 14;16 (8) :3018-3027.|Front Pharmacol. 2022 Feb 23:13:816133.|Front Pharmacol. 2022 Feb 23;13:816133.|Gen Comp Endocrinol. 2018 Oct 1:267:1-8.|Int J Biol Sci. 2024 Jul 15;20 (10) :3892-3910.|Int J Mol Med. 2021 Jan;47 (1) :302-314.|Int J Mol Sci. 2023 Mar 3;24 (5) :4921.|J Agric Food Chem. 2025 May 7;73 (18) :10998-11006.|J Clin Endocrinol Metab. 2024 Oct 16:dgae735.|J Food Sci. 2018 Sep;83 (9) :2394-2401.|J Tradit Complement Med. 2024 Jul 2.|J Vet Sci. 2018 Mar 31;19 (2) :179-187. |Neurosci Lett. 2025 Aug 9:865:138351.|Oxid Med Cell Longev. 2017:2017:3869561.|Oxid Med Cell Longev. 2021 Jan 12;2021:3010548.|Photochem Photobiol. 2022 Sep;98 (5) :1157-1166.|Phytomedicine. 2021 Apr:84:153507.|Sci Rep. 2025 May 9;15 (1) :16209.|Sci Rep. 2019 Dec 12;9 (1) :18979. |Toxicon. 2026 Jan:269:108660.|FASEB Bioadv. 2025 Sep 3;7 (8) :e70045.|University of Verona. 2025.

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