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