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BMS-470539 dihydrochloride

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Catalog No. T10568Cas No. 2341796-82-3
Alias BMS470539 dihydrochloride, BMS 470539 dihydrochloride

BMS-470539 dihydrochloride is a selective and highly potent melanocortin 1 receptor (MC-1 R) agonist with anti-inflammatory activity. BMS-470539 attenuates oxidative stress and neuronal apoptosis via the MC1R/cAMP/PKA/Nurr1 signaling pathway in a neonatal hypoxia-ischemia rat model.

BMS-470539 dihydrochloride

BMS-470539 dihydrochloride

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Catalog No. T10568Alias BMS470539 dihydrochloride, BMS 470539 dihydrochlorideCas No. 2341796-82-3
BMS-470539 dihydrochloride is a selective and highly potent melanocortin 1 receptor (MC-1 R) agonist with anti-inflammatory activity. BMS-470539 attenuates oxidative stress and neuronal apoptosis via the MC1R/cAMP/PKA/Nurr1 signaling pathway in a neonatal hypoxia-ischemia rat model.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$52In StockIn Stock
5 mg$123In StockIn Stock
10 mg$198In StockIn Stock
25 mg$455In StockIn Stock
50 mg$745In StockIn Stock
100 mg$1,180-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:>99.99%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
BMS-470539 dihydrochloride is a selective and highly potent melanocortin 1 receptor (MC-1 R) agonist with anti-inflammatory activity. BMS-470539 attenuates oxidative stress and neuronal apoptosis via the MC1R/cAMP/PKA/Nurr1 signaling pathway in a neonatal hypoxia-ischemia rat model.
Targets&IC50
MC1R:120 nM, MC1R:28 nM (EC50)
In vitro
METHODS: BMS-470539 dihydrochloride (0-1μM, 15 minutes) was used to treat HBL cells stably transfected with NF-B luciferase reporter gene, and then treated with 0.5 ng/mL TNF-α for 4 hours to study its effect on stable transfection. Effects of NF-B luciferase reporter gene on TNF-α-stimulated luciferase activation in HBL cells.
RESULTS:BMS-470539 dihydrochloride treatment of HBL cells with NF-B luciferase reporter gene caused a dose-dependent significant reduction in TNF-α-stimulated NF-B luciferase activity. [2]
In vivo
METHODS: BMS-470539 dihydrochloride (2.05-18.47 mg/kg, intravenous injection, 125 minutes) was used to treat WT and MC1 receptor-negative e/e mice to study its effects on mesenteric microcirculation.
RESULTS:BMS-470539 dihydrochloride treatment of mice inhibited cell adhesion and migration, had no effect on cell rolling, and also inhibited the tissue expression of two chemokines, CXCL1 and CCL2. [3]
SynonymsBMS470539 dihydrochloride, BMS 470539 dihydrochloride
Chemical Properties
Molecular Weight632.62
FormulaC32H43Cl2N5O4
Cas No.2341796-82-3
SmilesCCCC(C1(C2=CC=CC=C2)CCN(CC1)C([C@H](NC([C@@H](N)CC3=CN=CN3C)=O)CC4=CC=C(C=C4)OC)=O)=O.Cl.Cl
Relative Density.no data available
Storage & Solubility Information
Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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