NPS-2143 hydrochloride

SKU: orb1302409

Description

NPS-2143 hydrochloride

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 324523-20-8
• MW: 445.38
• Purity: 99.67%
• Formula: C₂₄H₂₅ClN₂O₂.HCl
• SMILES: Cl.CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1cccc(Cl)c1C#N
• Target: CaSR
• Solubility: DMSO:50 mg/mL (112.26 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.49 mM)

Bioactivity

• Target IC50:
  CaSR:43nM/41nM
• 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 . Concurrent administration with an antiresorptive agent (estradiol) resulted in enhanced trabecular bone volume and bone mineral density in osteopenic rats.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CaSR, Calcium-sensing receptor, NPS 2143, NPS 2143 Hydrochloride, NPS 2143 hydrochloride, NPS2143, NPS-2143, NPS-2143 HCL, NPS2143 Hydrochloride, NPS2143 hydrochloride, NPS-2143 Hydrochloride, inhibit, Inhibitor, SB-262470A

Compound Identifiers

PubChem CID

9868131