JNJ-10229570,524923-88-4

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JNJ-10229570

CAS No. : 524923-88-4

MCE 国际站：JNJ-10229570

产品活性：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。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Melanocortin Receptor

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.

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.

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