NPS-2143 (hydrochloride)

NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) 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

[324523-20-8]

Product Name Alternative

SB-262470A (hydrochloride)

UNSPSC

12352005

Hazard Statement

H302+H312+H332, H410

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-hydrochloride.html

Purity

99.98

Solubility

DMSO : ≥ 100 mg/mL|H2O : 1.85 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C24H26Cl2N2O2

Molecular Weight

445.38

Precautions

H302+H312+H332, H410

References & Citations

[1]Huang Y, Breitwieser GE. Rescue of calcium-sensing receptor mutants by allosteric modulators reveals a conformational checkpoint in receptor biogenesis. J Biol Chem. 2007 Mar 30;282 (13) :9517-25|[2]Marquis, Robert W.; Lago, Amparo M.; Callahan, James F.; Antagonists of the Calcium Receptor. 2. Amino Alcohol-Based Parathyroid Hormone Secretagogues. Journal of Medicinal Chemistry (2009), 52 (21), 6599-6605.|[3]Yamamura A, Guo Q, Yamamura H, Zimnicka AM, Pohl NM, Smith KA, Fernandez RA, Zeifman A, Makino A, Dong H, Yuan JX.Enhanced Ca2+-sensing receptor function in idiopathic pulmonary arterial hypertension.Circ Res. 2012 Aug 3;111 (4) :469-81. Epub 2012 Jun 22.|[4]Nakajima S, Hira T, Hara H.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]Davey AE, Leach K, Valant C, Conigrave AD, Sexton PM, Christopoulos A.Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor.Endocrinology. 2012 Mar;153 (3) :1232-41. Epub 2011 Dec 30.|[6]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.