NS 2028 | CAS#204326-43-2 | sGC Inhibitor

NS 2028
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 532366

CAS#: 204326-43-2

Description: NS 2028 is a potent soluble guanylyl cyclase (sGC) inhibitor (Ki = 8 nM). It blocks sGC activity in murine cerebellum induced by S-nitroso-glutathione and NMDA (IC50 values are 17 and 20 nM respectively). NS 2028 also inhibits VEGF-induced cGMP accumulation.

Chemical Structure

NS 2028

CAS# 204326-43-2

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 532366
Name: NS 2028
CAS#: 204326-43-2
Chemical Formula: C9H5BrN2O3
Exact Mass: 267.95
Molecular Weight: 269.054
Elemental Analysis: C, 40.18; H, 1.87; Br, 29.70; N, 10.41; O, 17.84

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 320
10mg	USD 550
25mg	USD 1100
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: NS 2028; NS-2028; NS2028.

IUPAC/Chemical Name: 8-bromo-4H-[1,2,4]oxadiazolo[3,4-c][1,4]benzoxazin-1-one

InChi Key: MUDRLQRJCGJJTB-UHFFFAOYSA-N

InChi Code: InChI=1S/C9H5BrN2O3/c10-5-1-2-7-6(3-5)12-8(4-14-7)11-15-9(12)13/h1-3H,4H2

SMILES Code: O=C1ON=C2COC3=CC=C(Br)C=C3N21

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:	NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity.
In vitro activity:	sh67LR lentivirus, anti67LR antibody, and cGMP inhibitor NS2028 were used to determine how a 67LR/cGMP signaling pathway regulated coptisine-induced apoptosis. cGMP inhibitor NS2028 significantly decreased coptisine-induced apoptosis and inhibition of cell viability. Reference: Front Pharmacol. 2018 May 18;9:517. https://pubmed.ncbi.nlm.nih.gov/29867512/
In vivo activity:	Rabbits receiving NS-2028 orally displayed a reduced angiogenic response to VEGF. As increased vascular permeability occurs prior to new blood vessel formation, this study determined the effect of NS-2028 in vascular leakage. Using a modified Miles assay, we observed that NS-2028 attenuated VEGF-induced permeability. Reference: Am J Physiol Regul Integr Comp Physiol. 2010 Mar;298(3):R824-32. https://pubmed.ncbi.nlm.nih.gov/20032260/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	138.5	514.60
	Ethanol	5.4	20.00

Preparing Stock Solutions

The following data is based on the product molecular weight 269.05 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. Zhou L, Yang F, Li G, Huang J, Liu Y, Zhang Q, Tang Q, Hu C, Zhang R. Coptisine Induces Apoptosis in Human Hepatoma Cells Through Activating 67-kDa Laminin Receptor/cGMP Signaling. Front Pharmacol. 2018 May 18;9:517. doi: 10.3389/fphar.2018.00517. PMID: 29867512; PMCID: PMC5968218. 2. Mülsch A, Bauersachs J, Schäfer A, Stasch JP, Kast R, Busse R. Effect of YC-1, an NO-independent, superoxide-sensitive stimulator of soluble guanylyl cyclase, on smooth muscle responsiveness to nitrovasodilators. Br J Pharmacol. 1997 Feb;120(4):681-9. doi: 10.1038/sj.bjp.0700982. PMID: 9051308; PMCID: PMC1564520. 3. Morbidelli L, Pyriochou A, Filippi S, Vasileiadis I, Roussos C, Zhou Z, Loutrari H, Waltenberger J, Stössel A, Giannis A, Ziche M, Papapetropoulos A. The soluble guanylyl cyclase inhibitor NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability. Am J Physiol Regul Integr Comp Physiol. 2010 Mar;298(3):R824-32. doi: 10.1152/ajpregu.00222.2009. Epub 2009 Dec 23. PMID: 20032260.
In vitro protocol:	1. Zhou L, Yang F, Li G, Huang J, Liu Y, Zhang Q, Tang Q, Hu C, Zhang R. Coptisine Induces Apoptosis in Human Hepatoma Cells Through Activating 67-kDa Laminin Receptor/cGMP Signaling. Front Pharmacol. 2018 May 18;9:517. doi: 10.3389/fphar.2018.00517. PMID: 29867512; PMCID: PMC5968218. 2. Mülsch A, Bauersachs J, Schäfer A, Stasch JP, Kast R, Busse R. Effect of YC-1, an NO-independent, superoxide-sensitive stimulator of soluble guanylyl cyclase, on smooth muscle responsiveness to nitrovasodilators. Br J Pharmacol. 1997 Feb;120(4):681-9. doi: 10.1038/sj.bjp.0700982. PMID: 9051308; PMCID: PMC1564520.
In vivo protocol:	1. Morbidelli L, Pyriochou A, Filippi S, Vasileiadis I, Roussos C, Zhou Z, Loutrari H, Waltenberger J, Stössel A, Giannis A, Ziche M, Papapetropoulos A. The soluble guanylyl cyclase inhibitor NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability. Am J Physiol Regul Integr Comp Physiol. 2010 Mar;298(3):R824-32. doi: 10.1152/ajpregu.00222.2009. Epub 2009 Dec 23. PMID: 20032260.

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1: Fang F, Pan M, Yan T, Tao Y, Wu H, Liu X, Qu J, Zhou X. The role of cGMP in ocular growth and the development of form-deprivation myopia in guinea pigs. Invest Ophthalmol Vis Sci. 2013 Dec 3;54(13):7887-902. doi: 10.1167/iovs.13-11999. PubMed PMID: 24130184.

2: Sawa T, Ihara H, Ida T, Fujii S, Nishida M, Akaike T. Formation, signaling functions, and metabolisms of nitrated cyclic nucleotide. Nitric Oxide. 2013 Nov 1;34:10-8. doi: 10.1016/j.niox.2013.04.004. Epub 2013 Apr 28. Review. PubMed PMID: 23632125.

3: Schallner N, Romão CC, Biermann J, Lagrèze WA, Otterbein LE, Buerkle H, Loop T, Goebel U. Carbon monoxide abrogates ischemic insult to neuronal cells via the soluble guanylate cyclase-cGMP pathway. PLoS One. 2013 Apr 8;8(4):e60672. doi: 10.1371/journal.pone.0060672. Print 2013. PubMed PMID: 23593279; PubMed Central PMCID: PMC3620383.

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