| Identification | Back Directory | [Name]
Hydrazinecarboximidamide, 2-[(2E)-3-[1-(2-nitrophenyl)-1H-pyrrol-2-yl]-2-propen-1-ylidene]-, (2E)- | [CAS]
1809420-71-0 | [Synonyms]
resomelagon
Hydrazinecarboximidamide, 2-[(2E)-3-[1-(2-nitrophenyl)-1H-pyrrol-2-yl]-2-propen-1-ylidene]-, (2E)- | [Molecular Formula]
C14H14N6O2 | [MOL File]
1809420-71-0.mol | [Molecular Weight]
298.3 |
| Chemical Properties | Back Directory | [Boiling point ]
513.0±60.0 °C(Predicted) | [density ]
1.35±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
8.85±0.70(Predicted) | [color ]
Light brown to brown |
| Hazard Information | Back Directory | [Uses]
Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research[1][2]. | [in vivo]
Resomelagon (0-10 mg/kg; i.p., i.v. and p.o.; for 24 h; male C57BL/6J wild-type (WT) and BALB/c mice) promotes resolution of acute inflammation in vivo[1].
Resomelagon (25-50 mg/kg; p.o.; daily, for 8 d; male C57BL/6J wild-type (WT) and BALB/c mice) reduces arthritis in mice[1]. | Animal Model: | Male C57BL/6J wild-type (WT) and BALB/c mice[1] | | Dosage: | 0, 0.1, 1 and 10 mg/kg | | Administration: | Oral administration, intraperitoneal injection and intravenous injection; for 24 hours | | Result: | Inhibited neutrophil and monocyte infiltration in a dose-dependent manner. |
| Animal Model: | Male C57BL/6J wild-type (WT) and BALB/c mice[1] | | Dosage: | 25 and 50 mg/kg | | Administration: | Oral administration; daily; for 8 days | | Result: | Reduced all signs of arthritis measured, including clinical score (-42%), paw swelling (-87%), proportion of animals with all four paws affected (-50%), and the severity of the inflammation (-70%). |
| [IC 50]
MC1R; MC3R | [References]
[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. DOI:10.4049/jimmunol.1402645
[2] WHO Drug Information. International Nonproprietary Names for Pharmaceutical |
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