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NS 2028

Alias: NS2028 NS-2028 NS 2028
Cat No.:V26664 Purity: ≥98%
NS-2028 is a selective soluble guanylate cyclase (sGC) inhibitor (antagonist) with IC50s of 30 nM and 200 nM for basal and NO-stimulated enzyme activities, respectively.
NS 2028
NS 2028 Chemical Structure CAS No.: 204326-43-2
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes
Official Supplier of:
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Product Description
NS-2028 is a selective soluble guanylate cyclase (sGC) inhibitor (antagonist) with IC50s of 30 nM and 200 nM for basal and NO-stimulated enzyme activities, respectively. NS-2028 inhibits soluble guanylyl cyclase activity in mouse cerebellar homogenate and neuronal NO synthase, with IC50s of 17 nM and 20 nM, respectively. NS-2028 inhibits the formation of cyclic GMP by 3-morpholino-sydnonimine (SIN-1) in human cultured umbilical vein endothelial cells with IC50 of 30 nM. NS-2028, commonly utilized in study/research of nitric oxide signaling pathways, completely inhibits NO-dependent relaxation responses in non-vascular smooth muscle (1μM). NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
When compared to cells cultured in a vehicle, NS -2028 (10 μM) suppresses cell number growth by 25% [2]. By preventing p38 MAPK activation, NS -2028 (10 μM; 30 min) stimulates cell proliferation test in the presence of VEGF [2].
ln Vivo
After VEGF particles were ingested, NS-2028 (a powder medication; 1 g/L; 8 days) dramatically decreased the formation of new blood vessels in avascular rabbits [2].
Cell Assay
Cell Proliferation Assay[2]
Cell Types: HUVEC Cell
Tested Concentrations: 10 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: diminished number of cells in culture. EC migration[2].

Western Blot Analysis[2]
Cell Types: HUVEC Cell
Tested Concentrations: 10 μM
Incubation Duration: 30 minutes
Experimental Results: VEGF-enhanced p38 phosphorylation is attenuated.
Animal Protocol
Animal/Disease Models: Rabbit[2]
Doses: 1 g/L
Route of Administration: Oral administration; 1 g/L; 8 days
Experimental Results: Inhibits VEGF-induced angiogenesis in vivo.
References

[1]. Characterization of NS 2028 as a specific inhibitor of soluble guanylyl cyclase. Br J Pharmacol. 1998 Jan;123(2):299-309.

[2]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C9H5BRN2O3
Molecular Weight
269.05
Exact Mass
267.948
CAS #
204326-43-2
PubChem CID
4551
Appearance
White to off-white solid powder
Density
2.1±0.1 g/cm3
Boiling Point
353.8±52.0 °C at 760 mmHg
Melting Point
161-162ºC
Flash Point
167.8±30.7 °C
Vapour Pressure
0.0±0.8 mmHg at 25°C
Index of Refraction
1.778
LogP
0.27
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
0
Heavy Atom Count
15
Complexity
333
Defined Atom Stereocenter Count
0
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
Chemical Name
8-bromo-4H-[1,2,4]oxadiazolo[3,4-c][1,4]benzoxazin-1-one
Synonyms
NS2028 NS-2028 NS 2028
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~250 mg/mL (~929.20 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.17 mg/mL (8.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.17 mg/mL (8.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.7168 mL 18.5839 mL 37.1678 mL
5 mM 0.7434 mL 3.7168 mL 7.4336 mL
10 mM 0.3717 mL 1.8584 mL 3.7168 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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