NPS2390 | CAS#226878-01-9 | mGlu antagonist

MedKoo Cat#: 532361 | Name: NPS2390

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

NPS2390 is a group I mGlu antagonist. It displays noncompetitive antagonist activity at both mGlu1 and mGlu5 receptors. NPS2390 is thought to act on a site separate from the glutamate binding pocket.

Chemical Structure

NPS2390

CAS#226878-01-9

Theoretical Analysis

MedKoo Cat#: 532361

Name: NPS2390

CAS#: 226878-01-9

Chemical Formula: C19H21N3O

Exact Mass: 307.1685

Molecular Weight: 307.40

Elemental Analysis: C, 74.24; H, 6.89; N, 13.67; O, 5.20

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 220.00
10mg	USD 390.00
25mg	USD 770.00

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Related CAS #

No Data

Synonym

NPS2390; NPS 2390; NPS-2390.

IUPAC/Chemical Name

N-(1-adamantyl)quinoxaline-2-carboxamide

InChi Key

ZKFVOZCCAXQXBU-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H21N3O/c23-18(17-11-20-15-3-1-2-4-16(15)21-17)22-19-8-12-5-13(9-19)7-14(6-12)10-19/h1-4,11-14H,5-10H2,(H,22,23)

SMILES Code

O=C(C1=NC2=CC=CC=C2N=C1)NC34CC5CC(C4)CC(C5)C3

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

NPS 2390 is a noncompetitive antagonist of mGluR1 and mGluR5.

In vitro activity:

The viability of human PASMCs was detected by cell cycle and BrdU. The results showed that hypoxia-induced autophagy was considerable at 24 h. The addition of NPS2390 decreased the expression of autophagy protein and synthetic phenotype marker protein osteopontin and increased the expression of contractile phenotype marker protein SMA-ɑ and calponin via suppressing downstream PI3K/Akt/mTOR signal pathways. This study demonstrates that treatment of NPS2390 was conducive to inhibit the proliferation and reverse phenotypic modulation of PASMCs by regulating autophagy levels. Reference: J Transl Int Med. 2019 Jul 11;7(2):59-68. https://pubmed.ncbi.nlm.nih.gov/31380238/

In vivo activity:

Rats were randomly distributed into three groups undergoing the sham surgery or TBI procedure, and NPS2390 (1.5 mg/kg) was infused subcutaneously at 30 min and 120 min after TBI. These data indicated that NPS2390 significantly reduced the brain edema and improved the neurological function after TBI. In addition, NPS2390 decreased caspase-3 levels and the number of apoptotic neurons. Furthermore, NPS2390 up-regulated anti-apoptotic protein Bcl-2 expression and down-regulated pro-apoptotic protein Bax, and reduced subsequent release of cytochrome c into the cytosol. Reference: Biochem Biophys Res Commun. 2017 Apr 29;486(2):589-594. https://pubmed.ncbi.nlm.nih.gov/28336431/

	Solvent	mg/mL	mM
Solubility
	Ethanol	7.8	25.41

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 307.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Peng X, Wei C, Li HZ, Li HX, Bai SZ, Wang LN, Xi YH, Yan J, Xu CQ. 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 Jul 11;7(2):59-68. doi: 10.2478/jtim-2019-0013. PMID: 31380238; PMCID: PMC6661874. 2. Li HX, Kong FJ, Bai SZ, He W, Xing WJ, Xi YH, Li GW, Guo J, Li HZ, Wu LY, Wang R, Yang GD, Tian Y, Xu CQ. Involvement of calcium-sensing receptor in oxLDL-induced MMP-2 production in vascular smooth muscle cells via PI3K/Akt pathway. Mol Cell Biochem. 2012 Mar;362(1-2):115-22. doi: 10.1007/s11010-011-1133-6. Epub 2011 Nov 15. PMID: 22083546. 3. Xue Z, Song Z, Wan Y, Wang K, Mo L, Wang Y. Calcium-sensing receptor antagonist NPS2390 attenuates neuronal apoptosis though intrinsic pathway following traumatic brain injury in rats. Biochem Biophys Res Commun. 2017 Apr 29;486(2):589-594. doi: 10.1016/j.bbrc.2017.03.097. Epub 2017 Mar 20. PMID: 28336431.

In vitro protocol:

In vivo protocol:

1. Xue Z, Song Z, Wan Y, Wang K, Mo L, Wang Y. Calcium-sensing receptor antagonist NPS2390 attenuates neuronal apoptosis though intrinsic pathway following traumatic brain injury in rats. Biochem Biophys Res Commun. 2017 Apr 29;486(2):589-594. doi: 10.1016/j.bbrc.2017.03.097. Epub 2017 Mar 20. PMID: 28336431.

1: Xue Z, Song Z, Wan Y, Wang K, Mo L, Wang Y. Calcium-sensing receptor antagonist NPS2390 attenuates neuronal apoptosis though intrinsic pathway following traumatic brain injury in rats. Biochem Biophys Res Commun. 2017 Apr 29;486(2):589-594. doi: 10.1016/j.bbrc.2017.03.097. Epub 2017 Mar 20. PubMed PMID: 28336431.