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JNJ-10229570
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ-10229570图片
CAS NO:524923-88-4
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
JNJ10229570
JNJ 10229570
UNII-N9IX402L35
产品介绍
JNJ-10229570 是肾上腺皮质受体 1 和肾上腺皮质受体 5 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。

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.

体外活性

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.

体内活性

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).?Treatment with flutamide, a known inhibitor of sebum production, the human skin/SCID mouse experimental system for sebaceous secretion studies

细胞实验

Radioligand binding assays were performed, with CHO-K1 cells over-expressing MC1R, and HEK-293 cells over-expressing MC4R or MC5R, using a single concentration of 125I-NDP-a-MSH and increasing concentrations of JNJ-7818369 or JNJ-10229570. IC50 values for inhibition of radioligand binding were calculated by a non-linear, least squares regression method.

动物实验

JNJ-10229570 (0.05%) and flutamide (5%) were dissolved in a vehicle of ethanol: propylene glycol (7:3).?20 ml/1.5 cm^2 were applied onto each skin xenograft, starting at three months posttransplantation.?Xenografts were treated once daily, 5 days/week, for 30 34 treatments.?Xenografts were then collected for histological examination and lipid analysis.?Each study was repeated with skin xenografts from at least 3 donors.?The vehicle had no effect on sebaceous glands differentiation or activity.

Cas No.

524923-88-4

分子式

C22H19N3O2S

分子量

389.47

别名

JNJ10229570;JNJ 10229570;UNII-N9IX402L35

储存和溶解度

DMSO:62.5 mg/mL (160.47 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years