JNJ-10229570

Research use only, not for human use.

JNJ-10229570 (JNJ10229570) is a novel potent, selective melanocortin receptor MC1R and MC5R antagonist with binding IC50 of 270 nM and 200 nM, respectively.

JNJ-10229570 (JNJ10229570) is a novel potent, selective melanocortin receptor MC1R and MC5R antagonist with binding IC50 of 270 nM and 200 nM, respectively; dose dependently inhibited the production of sebaceous lipids in cultured primary human sebocytes; Topical treatment with JNJ-10229570 of human skins transplanted onto SCID mice resulted 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).Other Indication Phase 2 Discontinued.

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.

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.

JNJ10229570 | JNJ 10229570

GPCR/G Protein

Melanocortin Receptor

Melanocortin Receptor

Other Indications

Other Disease

524923-88-4

389.47

C22H19N3O2S

>98% (HPLC)

DMSO : 62.5 mg/mL 160.47 mM

COC1=CC=CC=C1C2=N/C(SN2C3=CC=CC=C3OC)=N\C4=CC=CC=C4

Benzenamine, N-(2,3-bis(2-methoxyphenyl)-1,2,4-thiadiazol-5(2H)-ylidene)-

(-20℃)

With Ice Pack

≥ 2 years