货号	规格	价格	上海	北京	珠海	重庆	武汉
S88684-1mg促销	≥98%	￥376.00 ￥338.00 S88684-1mg ￥338.00 现货	10 10	-	-	-	-
S88684-5mg促销	≥98%	￥1530.00 ￥1380.00 S88684-5mg ￥1380.00 现货	10 10	-	-	-	-
S88684-10mg促销	≥98%	￥2880.00 ￥2590.00 S88684-10mg ￥2590.00 现货	10 10	-	-	-	-
S88684-25mg促销	≥98%	￥4710.00 ￥4240.00 S88684-25mg ￥4240.00 现货	10 10	-	-	-	-
S88684-50mg促销	≥98%	￥9260.00 ￥8330.00 S88684-50mg ￥8330.00 现货	10 10	-	-	-	-
S88684-100mg促销	≥98%	￥13800.00 ￥12500.00 S88684-100mg ￥12500.00 现货	4 4	-	-	-	-

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产品描述：

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

靶点：

IC50: 270 nM (human MC1R), 200 nM (human MC5R);MelanocortinReceptor

体外研究：

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

体内研究：

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

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.568 ml	12.838 ml	25.676 ml
5 mM	0.514 ml	2.568 ml	5.135 ml
10 mM	0.257 ml	1.284 ml	2.568 ml
50 mM	0.051 ml	0.257 ml	0.514 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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