JNJ-10229570 是肾上腺皮质受体 1 (MC1R) 和肾上腺皮质受体 5 (MC5R) 的拮抗剂，可抑制皮脂腺分化和皮质特异性脂质的产生，其抑制 ¹²⁵I-NDP-α-MSH 和人类细胞中 MC1R 和 MC5R 结合的 IC₅₀ 值分别为 270 nM 和 200 nM。

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 I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC 50 values of 270 nM and 200 nM, respectively.

Solid

IC50: 270 nM (human MC1R), 200 nM (human MC5R).

JNJ-10229570 dose dependently inhibits the production of sebaceous lipids in cultured primary human sebocytes. JNJ-7818369 inhibits the binding of I-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. has not independently confirmed the accuracy of these methods. They are for reference only.

Topical treatment with JNJ-10229570 of human skins transplanted onto SCID mice result in a marked decrease in sebum-specific lipid production, sebaceous glands 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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Eisinger M, et al. A melanocortin receptor 1 and 5 antagonist inhibits sebaceous gland differentiation and the production of sebum-specific lipids. J Dermatol Sci. 2011 Jul;63(1):23-32.

In Vitro: DMSO : 62.5 mg/mL (160.47 mM; Need ultrasonic)配制储备液