NPS-2143

SKU: orb1706434

Description

NPS-2143 (SB 262470A) is a potent and selective calcium-sensing receptor (CaSR) antagonist. It is widely used in biochemical and physiological research to investigate CaSR function in vitro and has been applied in animal models to study disorders of calcium homeostasis, such as hyperparathyroidism.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 284035-33-2
• MW: 408.92
• Purity: 99.56% (May vary between batches)
• Formula: C₂₄H₂₅ClN₂O₂
• SMILES: CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc1cccc(Cl)c1C#N
• Target: CaSR,Calcium Channel
• Solubility: DMSO:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  Ca2+ receptor:43 nM
• In Vivo:
  In normotensive rats, intravenous administration of NPS 2143 (1 mg/kg) significantly increased mean arterial pressure (MAP) in the presence of the parathyroid gland. Additionally, NPS 2143 induced a rapid 4-5 fold increase in plasma parathyroid hormone (PTH) levels and an instantaneous rise in plasma calcium (Ca2+) levels.
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• In Vitro:
  NPS 2143 stimulates the secretion of parathyroid hormone (PTH) from bovine parathyroid cells with an effective concentration (EC50) of 41 nM. Moreover, NPS 2143 inhibits the suppressive effect of the calcimimetic NPS R-467 on PTH secretion from bovine parathyroid cells and the inhibition of cAMP formation stimulated by isoproterenol in the presence of extracellular Ca2+. In HEK 293 cells expressing the human Ca2+ receptor, NPS 2143 blocks the increase in cytosolic Ca2+ concentration induced by receptor activation, with an inhibitory concentration (IC50) of 43 nM. Furthermore, in HEK-293 cells transiently expressing hCaSRs, NPS 2143 significantly inhibits the umami taste perception by effectively suppressing GSH (data not shown) and γ-Glu-Val-Gly activity.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB262470, SB-262470, SB-262470A, SB 262470, SB 262470A, Calcium-sensing receptor, CaSR, CalciumChannel, Calcium Channel, Ca(2+) receptor, inhibit, NPS 2143, NPS2143, NPS-2143, Inhibitor

Compound Identifiers

PubChem CID

6918446