NS 383 | CAS#309711-59-9 | ASIC blocker

MedKoo Cat#: 463295 | Name: NS 383

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Description:

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

NS 383 is an ASIC blocker. Inhibition was observed at heteromeric ASIC channels. It attenuates pathophysiological nociceptive behaviors in CFA-inflamed and CCI rats.

Chemical Structure

NS 383

CAS#309711-59-9

Theoretical Analysis

MedKoo Cat#: 463295

Name: NS 383

CAS#: 309711-59-9

Chemical Formula: C19H19N3O2

Exact Mass: 321.1477

Molecular Weight: 321.38

Elemental Analysis: C, 71.01; H, 5.96; N, 13.08; O, 9.96

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 450.00	2 Weeks
50mg	USD 1,250.00	2 Weeks

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Related CAS #

No Data

Synonym

NS 383; NS383; NS-383;

IUPAC/Chemical Name

(E)-8-ethyl-3-(hydroxyimino)-5-phenyl-1,3,6,7,8,9-hexahydro-2H-pyrrolo[3,2-h]isoquinolin-2-one

InChi Key

CHVQAXYXYIDNDC-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H19N3O2/c1-2-22-9-8-13-14(12-6-4-3-5-7-12)10-15-17(16(13)11-22)20-19(23)18(15)21-24/h3-7,10,24H,2,8-9,11H2,1H3,(H,20,21,23)

SMILES Code

CCN1CCC2=C(C1)C3=C(C=C2C4=CC=CC=C4)/C(C(N3)=O)=N\O

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

>3 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:

NS383 is a potent and uniquely selective inhibitor of rat ASICs containing 1a and/or 3 subunits.

In vitro activity:

NS383 likewise concentration‐dependently inhibited ASIC1a and ASIC3 currents with IC50 values of 0.44 and 2.1 μM, respectively. However, no robust inhibition was observed at homomeric ASIC2a (Figure 2B, Table 1). Compared with amiloride, NS383 is thus 10‐ to 30‐fold more potent and displays selectivity between ASIC subtypes. Interestingly, the inhibition by NS383 at ASIC1a and ASIC3 was affected by the stimulatory H+ concentration (Figure 2D). Reference: CNS Neurosci Ther. 2016 Feb;22(2):135-45. https://pubmed.ncbi.nlm.nih.gov/26663905/

In vivo activity:

Twenty‐four hours after hindpaw CFA injection, a marked alteration in hindpaw weight bearing indicative of spontaneous nonevoked pain was observed (44.4 ± 2.3 g vs. 5.2 ± 2.2 g prior to injection, n = 128, P < 0.001, Student's t‐test). This deficit was completely reversed by NS383 (10–60 mg/kg; F(3, 30) = 9.677, P < 0.001, amiloride (50–200 mg/kg; F(3, 31) = 4.958, P < 0.01), and acetaminophen (100–400 mg/kg; F(3, 31) = 4.195, P < 0.05) (Figure 5A–C). Reference: CNS Neurosci Ther. 2016 Feb;22(2):135-45. https://pubmed.ncbi.nlm.nih.gov/26663905/

	Solvent	mg/mL	mM
Solubility
	DMSO	1.6	5.00

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 321.38 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:

Munro G, Christensen JK, Erichsen HK, Dyhring T, Demnitz J, Dam E, Ahring PK. NS383 Selectively Inhibits Acid-Sensing Ion Channels Containing 1a and 3 Subunits to Reverse Inflammatory and Neuropathic Hyperalgesia in Rats. CNS Neurosci Ther. 2016 Feb;22(2):135-45. doi: 10.1111/cns.12487. Epub 2015 Dec 10. PMID: 26663905; PMCID: PMC6492852.

In vitro protocol:

In vivo protocol: