Molecular Formula | C24H26Cl2N2O2 |
Molar Mass | 445.38 |
Solubility | DMSO: >10mg/mL |
Appearance | powder |
Color | white to beige |
Storage Condition | 2-8°C |
In vitro study | NPS-2143 hydrochloride (SB-262470A hydrochloride) stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells with EC 50 of 41 nM. Moreover, NPS-2143 hydrochloride 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 vivo study | When infused intravenously in normal rats, NPS-2143 hydrochloride (SB-262470A hydrochloride) causes a rapid and large increase in plasma levels of PTH. Ca 2+ receptor antagonists are termed calcilytics and NPS-2143 is the first substance (either atomic or molecular) shown to possess such activity. When administered together with an antiresorptive agent (estradiol), NPS 2143 causes an increase in trabecular bone volume and bone mineral density in osteopenic rats. |
Risk Codes | R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. R50/53 - Very toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. |
Safety Description | S36/37 - Wear suitable protective clothing and gloves. S60 - This material and its container must be disposed of as hazardous waste. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
UN IDs | UN 3077 9 / PGIII |
WGK Germany | 3 |
biological activity | NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcium-dissolving agent, is a selective calcium-sensing receptor (CaSR). Antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) increases cytoplasmic Ca2 concentration by activating Ca2 receptors in HEK 293 cells that express human Ca2 receptors (IC50=43 nM). |