Powder: -20°C for 3 years
In solvent: -80°C for 2 years
JNJ-10229570 is an antagonist of <a href="/target/Melanocortin_Receptor" style="display: inline; color: #c13a36">Melanocortin Receptor</a> 1 (MC1R) and <a href="/target/Melanocortin_Receptor" style="display: inline; color: #c13a36">Melanocortin Receptor</a> 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 117.00 | |
5 mg | In stock | $ 239.00 | |
10 mg | In stock | $ 369.00 | |
25 mg | In stock | $ 790.00 | |
50 mg | In stock | $ 976.00 | |
100 mg | In stock | $ 1,381.00 | |
200 mg | In stock | $ 2,069.00 |
Description | 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. |
Targets&IC50 | human MC5R:200 nM, human MC1R:270 nM |
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 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 |
Cell Research | 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. |
Animal Research | 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. |
Synonyms | JNJ10229570, JNJ 10229570, UNII-N9IX402L35 |
Molecular Weight | 389.47 |
Formula | C22H19N3O2S |
CAS No. | 524923-88-4 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 62.5 mg/mL (160.47 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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JNJ-10229570 524923-88-4 GPCR/G Protein Neuroscience Melanocortin Receptor JNJ10229570 JNJ 10229570 MC Receptor Inhibitor inhibit UNII-N9IX402L35 inhibitor