Referencia número: HY-11095

NPS 2390

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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.

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Pureza: 99.90%
No. CAS: 226878-01-9
Fòrmula: C₁₉H₂₁N₃O
Peso molecular:307.40

Almacenamiento:

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)

NPS 2390 Chemical Structure

No. CAS: 226878-01-9

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Amount: USD 0.00

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[3]

mGluR1

5 nM ()

mGluR5

82 nM ()

Ver todos los productos específicos de isoformas mGluR :

Ver todos los productos específicos de isoformas PI3K :

Ver todos los productos específicos de isoformas Akt :

Ver todos los productos específicos de isoformas mTOR :

Ver todos los productos específicos de isoformas Bcl-2 Family :

Ver todos los productos específicos de isoformas Caspase :

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

human pulmonary arterial smooth muscle cells (HPASMCs)
Concentration:

10 µM
Incubation Time:

24 h (under hypoxia)
Result:

Increased the expression of phosphorylated PI3K, phosphorylated Akt, and phosphorylated mTOR, reversing the hypoxia-induced reduction in their phosphorylation levels.

In Vivo

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.

Animal Model:

Sprague Dawley (male, adult, 300-330 g, traumatic brain injury controlled cortical impact model)^[2]
Dosage:

1.5 mg/kg
Administration:

s.c.; twice (30 min and 120 min after TBI)
Result:

Significantly reduced brain water content compared to vehicle-treated TBI rats.
Significantly decreased modified neurological severity scores compared to vehicle-treated TBI rats.
Significantly reduced the number of TUNEL-positive neurons compared to vehicle-treated TBI rats.
Markedly diminished cleaved caspase-3 and Bax protein expression compared to vehicle-treated TBI rats.
Significantly increased Bcl-2 protein expression compared to vehicle-treated TBI rats.
Inhibited the release of cytochrome c into the cytosol compared to vehicle-treated TBI rats.

Chemical Information

No. CAS 226878-01-9
Appearance Solid
Peso molecular 307.40
Fòrmula C₁₉H₂₁N₃O
Color White to light yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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)

Solvente y solubilidad

In Vitro:

DMSO : 6.25 mg/mL (20.33 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2531 mL

16.2655 mL

32.5309 mL

5 mM

0.6506 mL

3.2531 mL

6.5062 mL

10 mM

0.3253 mL

1.6265 mL

3.2531 mL

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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (277 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2531 mL	16.2655 mL	32.5309 mL	81.3273 mL
	5 mM	0.6506 mL	3.2531 mL	6.5062 mL	16.2655 mL
	10 mM	0.3253 mL	1.6265 mL	3.2531 mL	8.1327 mL
	15 mM	0.2169 mL	1.0844 mL	2.1687 mL	5.4218 mL
	20 mM	0.1627 mL	0.8133 mL	1.6265 mL	4.0664 mL

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NPS 2390

Apoptosis Compound Library

GPCR/G Protein Compound Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Neurotransmitter Receptor Compound Library

Glutamine Metabolism Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Protease Inhibitor Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Lactylation Compound Library

MCE Kinase Hinge Binder Fragment Library

Ver todos los productos específicos de isoformas mGluR

Ver todos los productos específicos de isoformas PI3K

Ver todos los productos específicos de isoformas Akt

Ver todos los productos específicos de isoformas mTOR

Ver todos los productos específicos de isoformas Bcl-2 Family

Ver todos los productos específicos de isoformas Caspase

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

NPS 2390 Related Classifications

HY-11095 Related Classifications