AP1189 (acetate)

AP1189 is a biased agonist of melanocortin receptor 1 (MC1R) and MC3R. It induces ERK1 and ERK2 phosphorylation but not canonical cAMP production in HEK293 cells expressing human MC1R or MC3R when used at concentrations ranging from 10 pM to 1 mM. AP1189 (0.1-10 nM) reduces zymosan-induced IL-1beta, IL-6, and TNF-alpha production in primary peritoneal macrophages isolated from wild-type but not Mc3r-/- mice. It reduces zymosan-induced TNF-alpha production but has no effect on IL-1beta or IL-6 production in primary macrophages isolated from Mc1r-/- mice. AP1189 promotes efferocytosis in primary mouse macrophages. In vivo, AP1189 (1, 3, and 10 mg/kg) reduces peritoneal neutrophil infiltration in a mouse model of zymosan-induced acute peritonitis. AP1189 (50 mg/kg) reduces paw volume, the number of paws affected, and disease severity in a mouse model of arthritogenic serum-induced arthritis.Formal Name: 2-[3-[1-(2-nitrophenyl)-1H-pyrrol-2-yl]-2-propen-1-ylidene]-hydrazinecarboximidamide, acetate. CAS Number: 959850-74-9. Molecular Formula: C14H14N6O2 . C2H4O2. Formula Weight: 358.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 0.2 mg/ml. lambdamax: 350 nm. SMILES: O=C(C)O.N=C(N)NN=CC=CC1=CC=CN1C2=CC=CC=C2[N+]([O-])=O. InChi Code: InChI=1S/C14H14N6O2.C2H4O2/c15-14(16)18-17-9-3-5-11-6-4-10-19(11)12-7-1-2-8-13(12)20(21)22,1-2(3)4/h1-10H,(H4,15,16,18),1H3,(H,3,4). InChi Key: FIESOFUABUPMMH-UHFFFAOYSA-N.