| Bioactivity | Resomelagon (AP1189) acetate is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon acetate induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon acetate has anti-inflammatory activity. Resomelagon acetate can be used for obesity and chronic inflammation research[1][2]. |
| Target | Targrt: MC1 and MC3 |
| Invitro | Resomelagon acetate（0-1000 μM；8 分钟；HEK293A 细胞）通过 ERK1/2 磷酸化和 Ca2+ 动员促进黑皮质素信号转导[1] 。Resomelagon acetate（1 nM；30 分钟；腹膜巨噬细胞）具有抗炎活性并抑制 TNF-α 释放和胞吐作用[1]。 |
| In Vivo | Resomelagon acetate（0-10 mg/kg；腹腔注射、静脉注射、口服.；24 小时；雄性 C57BL/6J 野生型 (WT) 和 BALB/c 小鼠）促进体内急性炎症的消退[1 ]。Resomelagon acetate（25-50 mg/kg；口服；每日一次，持续 8 天；雄性 C57BL/6J 野生型 (WT) 和 BALB/c 小鼠）减少小鼠的关节炎[1]。 |
| Name | Resomelagon acetate |
| CAS | 1809420-72-1 |
| Formula | C16H18N6O4 |
| Molar Mass | 358.35 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Montero-Melendez T, et, al. Biased agonism as a novel strategy to harness the proresolving properties of melanocortin receptors without eliciting melanogenic effects. J Immunol. 2015 Apr 1;194(7):3381-8. [2]. WHO Drug Information. International Nonproprietary Names for Pharmaceutical. |
Resomelagon acetate
CAS: 1809420-72-1 F: C16H18N6O4 W: 358.35
Resomelagon (AP1189) acetate is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelago
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