NPS-2143

SKU: orb1225435

Description

A potent, selective and orally active CaSR antagonist with IC50 of 43 nM; does not inhibit cytoplasmic Ca2+ responses to glutamate in HEK 293 cells engineered to express mGluRs and GABAB receptors; stimulates parathyroid hormone (PTH ) secretion from bovine parathyroid cells in vitro (EC50=39 nM) and increases plasma PTH levels in vivo; also inhibits lipopolysaccharide-induced pulmonary inflammation.Osteoporosis Discontinued.

Research Area

Neuroscience

Key Properties

• CAS Number: 284035-33-2
• MW: 408.9205
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₅ClN₂O₂
• SMILES: CC(C)(CC1=CC2=CC=CC=C2C=C1)NC[C@H](COC3=C(C(=CC=C3)Cl)C#N)O
• Target: CaSR
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  NPS-2143 (SB-262470A) results in a rapid 4-to 5-fold increase in plasma PTH levels in rats. In normotensive rats, NPS-2143 administration (1 mg/kg, i. v.) markedly increases mean arterial blood pressure (MAP) in the presence of parathyroid glands.
• In Vitro:
  NPS-2143 (SB-262470A) stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells with EC50 of 41 nM. Moreover, NPS 214 also blocks the inhibitory effects of calcimimetic NPS R-467 on PTH secretion from bovine parathyroid cells and the inhibitory effects of extracellular Ca2+ on isoproterenol-stimulated increases in cyclic AMP formation. In HEK 293 cells transiently expressing hCaSRs, NPS-2143 significantly suppresses the kokumi taste by effectively inhibiting the activity of both GSH and γ-Glu-Val-Gly. A recent study shows that NPS-2143 treatment suppresses low molecular weight fractions of azuki hydrolysate-induced cholecystokinin (CCK) secretion in CaSR-transfected HEK 293 cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NPS 2143 | SB-262470 | NPS2143 | SB 262470

Quick Database Links

Gene Symbol

CaSR