NPS 2390
- Product Name
- NPS 2390
- CAS No.
- 226878-01-9
- Chemical Name
- NPS 2390
- Synonyms
- NPS2390, 10 mM in DMSO;N-(1-adamantyl)quinoxaline-2-carboxamide;N-(Adamantan-1-yl)quinoxaline-2-carboxamide;N-tricyclo[3.3.1.13,7]dec-1-yl-2-quinoxalinecarboxamide;2-Quinoxalinecarboxamide, N-tricyclo[3.3.1.13,7]dec-1-yl-;Inhibitor,NPS2390,Calcium-sensing receptor,NPS-2390,mGluR,inhibit,Metabotropic glutamate receptors,CaSR,NPS 2390
- CBNumber
- CB0972884
- Molecular Formula
- C19H21N3O
- Formula Weight
- 307.39
- MOL File
- 226878-01-9.mol
NPS 2390 Property
- Boiling point:
- 542.4±30.0 °C(Predicted)
- Density
- 1.28±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- Soluble to 50 mM in DMSO and to 50 mM in ethanol
- form
- Powder
- pka
- 11.53±0.20(Predicted)
- color
- White to light yellow
N-Bromosuccinimide Price
- Product number
- 11989
- Product name
- NPS 2390
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $89
- Updated
- 2024/03/01
- Product number
- 11989
- Product name
- NPS 2390
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $168
- Updated
- 2024/03/01
- Product number
- 11989
- Product name
- NPS 2390
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $395
- Updated
- 2024/03/01
- Product number
- N899033
- Product name
- NPS2390
- Packaging
- 1mg
- Price
- $45
- Updated
- 2021/12/16
- Product number
- N899033
- Product name
- NPS2390
- Packaging
- 5mg
- Price
- $75
- Updated
- 2021/12/16
NPS 2390 Chemical Properties,Usage,Production
Description
Metabotropic glutamate receptors (mGluRs), mediate excitatory synaptic transmission in the central nervous system. Potent and selective antagonists of the type I mGluRs (mGluR1 and mGluR5) are of interest as novel therapeutics for the treatment of various CNS disorders, such as pain, epilepsy, and stroke. NPS 2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 with IC50 values equal to 5.2 and 82 nM, respectively). At concentrations up to 30 μM, NPS 2390 does not affect mGluR2 or mGluR8 or a standard collection of 37 additional receptors, ion channels, and enzymes. At a dose of 10 mg/kg, NPS 2390 displaced the specifically bound mGlu1R-
Uses
Metabotropic glutamate receptors (mGluRs), mediate excitatory synaptic transmission in the central nervous system. Potent and selective antagonists of the type I mGluRs (mGluR1 and mGluR5) are of interest as novel therapeutics for the treatment of various CNS disorders, such as pain, epilepsy, and stroke. NPS 2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 with IC50 values equal to 5.2 and 82 nM, respectively). At concentrations up to 30 μM, NPS 2390 does not affect mGluR2 or mGluR8 or a standard collection of 37 additional receptors, ion channels, and enzymes. At a dose of 10 mg/kg, NPS 2390 displaced the specifically bound mGlu1R-selective antagonist, [3H]R214127, in rat cerebellum.
Uses
NPS 2390 is an inhibitor of CaSR (Calcium-sensing recpetor). NPS 2390 up-regulated anti-apoptotic protein Bcl-2 expression and down-regulated pro-apoptotic protein Bax.
IC 50
mGluR1; mGluR5
storage
Store at RT
References
[1] FRANCESCO FERRAGUTI F N Luca Crepaldi. Metabotropic glutamate 1 receptor: current concepts and perspectives.[J]. Pharmacological Reviews, 2008, 60 4: 536-581. DOI: 10.1124/pr.108.000166
[2] DOMINIQUE MABIRE. Synthesis, Structure?Activity Relationship, and Receptor Pharmacology of a New Series of Quinoline Derivatives Acting as Selective, Noncompetitive mGlu1 Antagonists[J]. Journal of Medicinal Chemistry, 2005, 48 6: 2134-2153. DOI: 10.1021/jm049499o
[3] De Souza, F.I., Zumiotti, A.V., and Da Silva, C.F. Neuregulins 1-α and 1-β on the regeneration the peripheral nerves[J]. Acta Ortop Bras.
[4] HILDE LAVREYSEN. [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.[J]. Molecular Pharmacology, 2003, 63 5: 1082-1093. DOI: 10.1124/mol.63.5.1082
NPS 2390 Preparation Products And Raw materials
Raw materials
Preparation Products
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