NPS 2390 

NPS 2390 is an allosteric antagonist of calcium-sensing receptor (CaSR) and mGluR1/5. NPS 2390 inhibits the PI3K/Akt/mTOR signaling pathway, reduces hypoxia-induced intracellular calcium elevation, decreases the expression of autophagy (autophagy) proteins, regulates the expression of phenotypic marker proteins, and inhibits the proliferation of pulmonary artery smooth muscle cells. NPS 2390 attenuates the endogenous apoptosis (apoptosis) pathway, increases the expression level of Bcl-2, downregulates the expression levels of Bax, cytochrome c and caspase-3, alleviates cerebral edema and improves neurological function in rat models. NPS 2390 can be used in studies related to hypoxic pulmonary hypertension, traumatic brain injury, stroke and pain^[1][2][3].

NPS 2390 (10 µM; 24 h) inhibits hypoxia-induced proliferation and reverses phenotypic modulation in human pulmonary arterial smooth muscle cells by reducing autophagy levels^[1].
NPS 2390 (10 µM; 24 h) suppresses hypoxia-induced increases in intracellular calcium concentration in human pulmonary arterial smooth muscle cells^[1].
NPS 2390 (10 µM; 24 h) activates the PI3K/Akt/mTOR signaling pathway in hypoxic human pulmonary arterial smooth muscle cells, which mediates its autophagy-inhibiting effects^[1].
NPS 2390 (multiple concentrations; 45 min) potently inhibits mGluR1 activity in rat cerebellar granule cells with an IC₅₀ of 0.005 μM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NPS 2390 (1.5 mg/kg; s.c.; twice (30 min and 120 min after TBI)) attenuates cortical neuronal apoptosis, alleviates brain edema, and improves neurological function following traumatic brain injury in Rattus norvegicus via modulation of the intrinsic apoptotic pathway^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

307.40

C₁₉H₂₁N₃O

226878-01-9

Solid

White to light yellow

O=C(NC1(C[C@@H]2C3)C[C@H](C2)C[C@H]3C1)C4=NC5=CC=CC=C5N=C4

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Peng X, et al. NPS2390, a Selective Calcium-sensing Receptor Antagonist Controls the Phenotypic Modulation of Hypoxic Human Pulmonary Arterial Smooth Muscle Cells by Regulating Autophagy. J Transl Int Med. 2019;7(2):59-68. Published 2019 Jul 11.  [Content Brief]

  [2]. Xue Z, et al. Calcium-sensing receptor antagonist NPS2390 attenuates neuronal apoptosis though intrinsic pathway following traumatic brain injury in rats. Biochem Biophys Res Commun. 2017;486(2):589-594.  [Content Brief]

  [3]. Vanejevs M, et al. Positive and negative modulation of group I metabotropic glutamate receptors. J Med Chem. 2008 Feb 14;51(3):634-47.  [Content Brief]