1809420-71-0

Name	Hydrazinecarboximidamide, 2-[(2E)-3-[1-(2-nitrophenyl)-1H-pyrrol-2-yl]-2-propen-1-ylidene]-, (2E)-
CAS	1809420-71-0
Molecular Formula	C14H14N6O2
Molecular Weight	298.3
MOL File	1809420-71-0.mol

Synonyms

resomelagon Hydrazinecarboximidamide, 2-[(2E)-3-[1-(2-nitrophenyl)-1H-pyrrol-2-yl]-2-propen-1-ylidene]-, (2E)-

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Chemical Properties

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

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

Supplier

Shanghai Yifei Biotechnology Co. , Ltd.

Telephone021-65675885 18964387627

Websitehttp://www.efebio.com

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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