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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $108 | 5 days | |
25 mg | $734 | 6-8 weeks | |
50 mg | $954 | 6-8 weeks | |
100 mg | $1,740 | 6-8 weeks |
Description | BMS-470539 dihydrochloride is a highly potent and selective agonist of the melanocortin-1 receptor (MC-1R; IC50: 120 nM; EC50: 28 nM) with anti-inflammatory properties. It does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. |
In vitro | An established HBL melanoma cell line stably expresses an NF-κB luciferase reporter, allowing for the observation that TNF-α at 0.5 ng/mL incites a dose-dependent escalations in NF-κB luciferase activity. Administering BMS-470539 to these HBL-NF-κB cells leads to a dose-dependent diminution in TNF-α-induced NF-κB luciferase activity, while it remains ineffective in altering luciferase reporter activity in the absence of TNF-α induction. In nontransfected HBL cells, BMS-470539 administration shows a dose-dependent deterrence of NF-κB nuclear translocation. |
In vivo | The treatment of BMS-470539 (2.05-18.47 mg/kg; i.v.; for 125 minutes; WT and MC1 receptor recessive e/e mice) inhibits cell emigration and adhesion with no effect on cell rolling. It also inhibits the tissue expression of CXCL1/CCL2 [3]. |
Molecular Weight | 596.17 |
Formula | C32H42ClN5O4 |
Cas No. | 2341796-82-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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