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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 Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $52 | In Stock | |
5 mg | $123 | In Stock | |
10 mg | $198 | In Stock | |
25 mg | $455 | In Stock | |
50 mg | $745 | In Stock | |
100 mg | $1,180 | In Stock |
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] |
Alias | BMS470539 dihydrochloride, BMS 470539 dihydrochloride |
Molecular Weight | 632.62 |
Formula | C32H43Cl2N5O4 |
Cas No. | 2341796-82-3 |
Smiles | CCCC(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 | store 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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