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NPS-2143 hydrochloride

Catalog No. T4967 CAS 324523-20-8

Synonyms: NPS-2143 HCL

NPS-2143 hydrochloride (NPS-2143 HCL) is a selective potent calcium ion-sensing receptor antagonist.

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NPS-2143 hydrochloride Chemical Structure

NPS-2143 hydrochloride, CAS 324523-20-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 84.00
10 mg	In stock	$ 128.00
25 mg	In stock	$ 226.00
50 mg	In stock	$ 356.00
100 mg	In stock	$ 528.00
1 mL * 10 mM (in DMSO)	In stock	$ 92.00

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Purity: 99.38%

Purity: 99.22%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	NPS-2143 hydrochloride (NPS-2143 HCL) is a selective potent calcium ion-sensing receptor antagonist.
Targets&IC50	CaSR:43nM/41nM
In vitro	NPS 2143, even when tested at much higher concentrations (3 microM), did not affect the activity of a number of other G protein-coupled receptors, including those most structurally homologous to the Ca2+ receptor. NPS 2143 stimulated parathyroid hormone (PTH) secretion from bovine parathyroid cells (EC50 of 41 nM) over a range of extracellular Ca2+ concentrations and reversed the effects of the calcimimetic compound NPS R-467 on [Ca2+]i and on secretion of PTH . The first reported calcilytic compound was NPS 2143, an orally active molecule which elicits rapid, 3- to 4-fold increases in circulating levels of PTH.
In vivo	When intravenously administered to normal rats, NPS 2143 swiftly elevated plasma PTH levels significantly. Known as calcilytics, substances like NPS 2143 act as Ca2+ receptor antagonists, with it being the inaugural compound (either atomic or molecular) identified with this activity [1]. Concurrent administration with an antiresorptive agent (estradiol) resulted in enhanced trabecular bone volume and bone mineral density in osteopenic rats.

Synonyms	NPS-2143 HCL
Molecular Weight	445.38
Formula	C24H25ClN2O2.HCl
CAS No.	324523-20-8

Storage

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

Solubility Information

DMSO: 50 mg/mL (112.26 mM)

References and Literature

1. 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. 2. 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. 3. 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. 4. 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 5. 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library GPCR Compound Library Bioactive Compound Library Preclinical Compound Library Target-Focused Phenotypic Screening Library Orally Active Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Anti-Metabolism Disease Compound Library Anti-COVID-19 Compound Library

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Keywords

NPS-2143 hydrochloride 324523-20-8 GPCR/G Protein CaSR NPS2143 NPS 2143 Hydrochloride NPS2143 Hydrochloride NPS-2143 NPS 2143 hydrochloride Calcium-sensing receptor inhibit SB-262470A Inhibitor NPS-2143 Hydrochloride NPS 2143 NPS-2143 HCL NPS2143 hydrochloride inhibitor

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