JNJ-10229570

JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R), MC4R, and MC5R (IC50s = 270, 240, and 200 nM, respectively, in radioligand binding assays). It prevents bovine pituitary extract-induced increases in lipid droplets in primary human sebocytes when used at a concentration of 0.05 µM. JNJ-10229570 (1 µM) inhibits cholera toxin-induced increases in squalene and cholesterol esters, but not triglycerides, in primary human sebocytes. Topical application of JNJ-10229570 (0.05%) inhibits sebum secretion from, and sebaceous gland differentiation in, transplanted human skin in a mouse xenograft model.Formal Name: N-[2,3-bis(2-methoxyphenyl)-1,2,4-thiadiazol-5(2H)-ylidene]-benzenamine. CAS Number: 524923-88-4. Molecular Formula: C22H19N3O2S. Formula Weight: 389.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: COC1=CC=CC=C1C(N(C2=CC=CC=C2OC)S3)=NC3=NC4=CC=CC=C4. InChi Code: InChI=1S/C22H19N3O2S/c1-26-19-14-8-6-12-17(19)21-24-22(23-16-10-4-3-5-11-16)28-25(21)18-13-7-9-15-20(18)27-2/h3-15H,1-2H3. InChi Key: XTHRTBCPBWJYRO-UHFFFAOYSA-N.