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LY83583

Alias: LY 83583; LY-83583; LY83583
Cat No.:V24725 Purity: ≥98%
LY83583 (LY 83583; LY-83583) is a novel and potent inhibitor of multple target proteins such as Msp1 and guanylate cyclase, also acts as a cGMP modulator that inhibits cGMP production.
LY83583
LY83583 Chemical Structure CAS No.: 91300-60-6
Product category: Guanylate Cyclase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
25mg
50mg
100mg
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Product Description
LY83583 (LY 83583; LY-83583) is a novel and potent inhibitor of multple target proteins such as Msp1 and guanylate cyclase, also acts as a cGMP modulator that inhibits cGMP production.
LY83583 is a soluble guanylate cyclase (sGC) competitive inhibitor with an IC50 of 2 μM. It targets the cGMP signaling pathway by inhibiting the conversion of GTP to cGMP. The compound inhibits the kinase activity-related proliferation of tumor cells by inducing the Cdk inhibitor p21.
Biological Activity I Assay Protocols (From Reference)
Targets
LY83583 targets soluble guanylate cyclase (sGC). It acts as a competitive inhibitor of this enzyme, which is responsible for converting GTP to cGMP. The compound also blocks the release of intracellular Ca2+ and antigen-induced leukotrienes.
ln Vitro
LY83583 inhibits soluble guanylate cyclase with an IC50 of 2 μM. It has been shown to inhibit leukotriene synthesis in guinea pig lung and rat peritoneal cells in vitro. The compound also blocks the release of intracellular Ca2+ and antigen-induced leukotrienes.
ln Vivo
In vivo, LY83583 inhibits cGMP production and modulates cGMP-mediated signaling pathways. The compound has been used to study the role of the nitric oxide-cGMP pathway in various physiological and pathological processes. Its effects on tumor cell proliferation have been investigated.
Enzyme Assay
In vitro enzyme assays measure the activity of soluble guanylate cyclase by monitoring the conversion of GTP to cGMP. LY83583 is incubated with purified sGC or tissue homogenates, and cGMP production is measured by radioimmunoassay or ELISA. The IC50 is determined from the inhibition of enzyme activity.
Cell Assay
In vitro cellular assays evaluate the effects of LY83583 on cGMP levels in cultured cells. Cells are treated with the compound, and intracellular cGMP is measured by immunoassay. The compound's effects on cell proliferation and p21 expression are also assessed in cancer cell lines. Calcium mobilization and leukotriene release assays may also be performed.
Animal Protocol
In vivo animal experiments are conducted to study the role of the cGMP pathway in various physiological processes. LY83583 is administered via intraperitoneal or intravenous injection. cGMP levels in tissues are measured, and physiological responses such as vasodilation or platelet aggregation are assessed.
ADME/Pharmacokinetics
LY83583 has a molecular formula of C15H10N2O2 and is also known as 6-anilino-5,8-quinolinequinone. It has a molecular weight of approximately 250.26. The compound is soluble in DMSO. It should be stored at -20°C. The compound has a purity of ≥95%.
Toxicity/Toxicokinetics
The toxicity profile of LY83583 is consistent with its mechanism as a guanylate cyclase inhibitor. Inhibition of cGMP production can affect multiple physiological processes including vasodilation and platelet function. The compound is used primarily as a research tool and its toxicity has been evaluated in the context of preclinical studies.
References

[1]. LY 83583 (6-anilino-5,8-quinolinedione) blocks nitrovasodilator-induced cyclic GMP increases and inhibition of platelet activation. Naunyn Schmiedebergs Arch Pharmacol. 1989 Jul;340(1):119-25.

Additional Infomation
6-Aniline-5,8-quinolinedione is a quinolone compound with the structure quinolin-5,8-dione, where the hydrogen at the 6-position is replaced by an aniline group. It possesses antitumor activity and is also an EC 4.6.1.2 (guanylate cyclase) inhibitor. It belongs to the quinolone class, aminoquinoline class, aromatic amine class, and is a paraquinone compound.
LY83583 is a biochemical compound used primarily in research to study the regulation of cGMP levels in cells. It is also known as 6-anilinoquinoline-5,8-quinone. The compound has been used to investigate the role of the nitric oxide-cGMP pathway in various physiological and pathological processes.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H10N2O2
Molecular Weight
250.25
Exact Mass
250.074
Elemental Analysis
C, 71.99; H, 4.03; N, 11.19; O, 12.79
CAS #
91300-60-6
PubChem CID
3976
Appearance
Brown to red solid powder
Density
1.4±0.1 g/cm3
Boiling Point
446.9±45.0 °C at 760 mmHg
Melting Point
184-185°C
Flash Point
224.1±28.7 °C
Vapour Pressure
0.0±1.1 mmHg at 25°C
Index of Refraction
1.715
LogP
1.56
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
2
Heavy Atom Count
19
Complexity
410
Defined Atom Stereocenter Count
0
SMILES
O=C1C2C(=CC=CN=2)C(=O)C(NC2C=CC=CC=2)=C1
InChi Key
GXIJYWUWLNHKNW-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H10N2O2/c18-13-9-12(17-10-5-2-1-3-6-10)15(19)11-7-4-8-16-14(11)13/h1-9,17H
Chemical Name
6-anilinoquinoline-5,8-dione
Synonyms
LY 83583; LY-83583; LY83583
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

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
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: ~200 mg/mL (~799.2 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.9960 mL 19.9800 mL 39.9600 mL
5 mM 0.7992 mL 3.9960 mL 7.9920 mL
10 mM 0.3996 mL 1.9980 mL 3.9960 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

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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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:
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  • 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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