JNJ-10229570

Cas No.:	524923-88-4
Chemical Name:	Benzenamine, N-(2,3-bis(2-methoxyphenyl)-1,2,4-thiadiazol-5(2H)-ylidene)-
Synonyms:	JNJ-10229570;JNJ 10229570;N9IX402L35;JNJ10229570;Benzenamine, N-(2,3-bis(2-methoxyphenyl)-1,2,4-thiadiazol-5(2H)-ylidene)-;2,3-bis(2-methoxyphenyl)-N-phenyl-1,2,4-thiadiazol-5-imine;BCP30848;ZVA92388;A16876;N16878;JNJ10229570; JNJ 10229570;Q27284735;2,3-Bis(2-methoxyphenyl)-N-phenyl-1,2,4-thiadiazol-5(2H)-imine
SMILES:	S1/C(=N/C2C([H])=C([H])C([H])=C([H])C=2[H])/N=C(C2=C([H])C([H])=C([H])C([H])=C2OC([H])([H])[H])N1C1=C([H])C([H])=C([H])C([H])=C1OC([H])([H])[H]
Formula:	C22H19N3O2S
M.Wt:	389.4702
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.
In Vivo:	Topical treatment with JNJ-10229570 of human skins transplanted onto SCID mice result in a marked decrease in sebum-specific lipid production, sebaceous gland's size and the expression of the sebaceous differentiation marker epithelial-membrane antigen (EMA). Topical treatment with 0.05% JNJ-10229570 leads to a distinct reduction in both the steady-state and the newly-synthesized sebum-specific lipids, with lesser effects on triglycerides and cholesterol[1].
In Vitro:	JNJ-10229570 dose dependently inhibits the production of sebaceous lipids in cultured primary human sebocytes. JNJ-7818369 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50s of 270±120 and 200±50 nM, respectively. Nearly-identical results are obtained with the free base form of the compound. Binding to MC4R of both forms of the compound is equipotent, with IC50s of 240±170 nM. JNJ-10229570-treated cells show strong inhibition of lipid granules at 0.01 μM, and complete inhibition at 0.05 μM[1].