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BMS-470539 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.
Catalog No. T10568Cas No. 2341796-82-3

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BMS-470539 dihydrochloride

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.
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Pack SizePriceAvailabilityQuantity
1 mg$526-8 weeks
5 mg$1236-8 weeks
10 mg$1986-8 weeks
25 mg$4556-8 weeks
50 mg$7456-8 weeks
100 mg$1,1806-8 weeks
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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]
AliasBMS470539 dihydrochloride, BMS 470539 dihydrochloride
Chemical Properties
Molecular Weight632.62
FormulaC32H43Cl2N5O4
Cas No.2341796-82-3
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.

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