Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Resomelagon (AP1189) is a potent, orally active agonist of melanocortin receptor (MR) that induces Ca2+ mobilization and ERK1/2 phosphorylation. Resomelagon shows anti-inflammatory activity that can be used in obesity and chronic inflammation research [1] [2].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 766.00 | |
50 mg | 6-8 weeks | $ 996.00 | |
100 mg | 6-8 weeks | $ 1,740.00 |
Description | Resomelagon (AP1189) is a potent, orally active agonist of melanocortin receptor (MR) that induces Ca2+ mobilization and ERK1/2 phosphorylation. Resomelagon shows anti-inflammatory activity that can be used in obesity and chronic inflammation research [1] [2]. |
In vitro | Resomelagon (AP1189), across concentrations ranging from 0-1000 µM for an 8-minute duration in HEK293A cells, enhances melanocortin signaling by inducing ERK1/2 phosphorylation and facilitating Ca2+ mobilization. Additionally, at a concentration of 1 nM over 30 minutes in peritoneal macrophages, it exhibits anti-inflammatory properties by inhibiting the release of TNF-α and suppressing efferocytosis. Western Blot analysis confirms that in HEK293A cells, ERK1/2 phosphorylation expression escalates in a dose-dependent manner, further supporting its role in activating these cellular pathways. |
In vivo | Resomelagon (AP1189), administered at doses ranging between 0-10 mg/kg through intraperitoneal, intravenous, and oral routes to male C57BL/6J wild-type (WT) and BALB/c mice over a period of 24 hours, effectively promotes acute inflammation resolution in vivo. At higher doses of 25-50 mg/kg, taken orally daily for 8 days, it significantly reduces arthritis symptoms in these mouse models. These effects include dose-dependent inhibition of neutrophil and monocyte infiltration and a marked reduction in arthritis symptoms, evidenced by lower clinical scores (42% decrease), reduced paw swelling (87% reduction), a lesser number of animals with all four paws affected (50% decrease), and decreased severity of inflammation (70% reduction). |
Molecular Weight | 298.3 |
Formula | C14H14N6O2 |
CAS No. | 1809420-71-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Resomelagon 1809420-71-0 inhibitor inhibit