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About This Item
Empirical Formula (Hill Notation):
C24H25ClN2O2 · HCl
CAS Number:
Molecular Weight:
445.38
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Product Name
NPS2143 hydrochloride, ≥98% (HPLC)
Quality Level
assay
≥98% (HPLC)
form
powder
optical activity
[α]20/D +20 to +24°, c = 1.0 in methanol
storage condition
desiccated
color
white to beige
solubility
DMSO: >10 mg/mL
storage temp.
2-8°C
SMILES string
Cl.CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc3cccc(Cl)c3C#N
InChI
1S/C24H25ClN2O2.ClH/c1-24(2,13-17-10-11-18-6-3-4-7-19(18)12-17)27-15-20(28)16-29-23-9-5-8-22(25)21(23)14-26;/h3-12,20,27-28H,13,15-16H2,1-2H3;1H/t20-;/m1./s1
InChI key
ZEBNDUQLNGYBNL-VEIFNGETSA-N
Application
NPS2143 hydrochloride has been used to study the function of calcium-sensing receptor :
- In the regulation of intestinal calcium transport.
- In the regulation of local negative feedback of intestinal calcium absorption.
- In sensorimotor decision making during development.
Biochem/physiol Actions
NPS2143 is a phenylalkylamine calcilytic compound, and might be useful in treating autosomal dominant hypocalcemia. It serves as a blocking agent for hERG (human ether-a-go-go-related gene ) channel, CYP2D6 (cytochrome P450 2D6 ) and monoamine transporters.
NPS2143 is a selective calcium-sensing receptor (CaR) antagonist.
NPS2143 is a selective calcium-sensing receptor (CaR) antagonist. The compound blocks increases in cytoplasmic calcium concentrations with an IC50 of 43 nM, and stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells over a wide range of extracellular calcuim concentrations.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Dermal - Acute Tox. 4 Inhalation - Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Novel activating mutations of the calcium-sensing receptor: the calcilytic NPS-2143 mitigates excessive signal transduction of mutant receptors
Letz S, et al.
The Journal of Clinical Endocrinology and Metabolism, 95(10), E229-E233 (2010)
Activation of calcium-sensing receptor by allosteric agonists cinacalcet and AC-265347 abolishes the 1, 25 (OH) 2D3-induced Ca2+ transport: Evidence that explains how the intestine prevents excessive Ca2+ absorption
Wongdee K, et al.
Archives of Biochemistry and Biophysics, 657, 15-22 (2018)
Progress in Medicinal Chemistry, 57 (2018)
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML0362-25MG | 04061833222546 |
| SML0362-5MG | 04061837084386 |

