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JNJ-10229570

Catalog No. T5464 CAS 524923-88-4

Synonyms: JNJ10229570, UNII-N9IX402L35, JNJ 10229570

JNJ-10229570 (UNII-N9IX402L35) 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.

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JNJ-10229570, CAS 524923-88-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 112.00
5 mg	In stock	$ 239.00
10 mg	In stock	$ 372.00
25 mg	In stock	$ 629.00
50 mg	In stock	$ 896.00
100 mg	In stock	$ 1,220.00
1 mL * 10 mM (in DMSO)	In stock	$ 263.00

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Purity: 99.06%

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Description	JNJ-10229570 (UNII-N9IX402L35) 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	MC5R (human):200 nM, MC1R (human):270 nM
In vitro	JNJ-10229570 demonstrates dose-dependent inhibition of sebaceous lipid production in cultured primary human sebocytes. Concurrently, JNJ-7818369 effectively prevents the attachment of 125I-NDP-α-MSH to cells featuring human MC1R and MC5R receptors, presenting IC50 values of 270±120 nM and 200±50 nM, respectively. Similar efficacy is observed with the compound's free base form. For both variations of the compound, the inhibitory action on MC4R is identical, with IC50 values reported at 240±170 nM. Notably, treatment with JNJ-10229570 at a concentration of 0.01 μM markedly suppresses lipid granule formation, achieving total inhibition at a concentration of 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, UNII-N9IX402L35, JNJ 10229570
Molecular Weight	389.47
Formula	C22H19N3O2S
CAS No.	524923-88-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 62.5 mg/mL (160.47 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Neuronal Signaling Compound Library Bioactive Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Anti-Obesity Compound Library Membrane Protein-targeted Compound Library GPCR Compound Library Inhibitor Library

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Keywords

JNJ-10229570 524923-88-4 GPCR/G Protein Neuroscience Melanocortin Receptor MC Receptor Inhibitor inhibit JNJ10229570 UNII-N9IX402L35 JNJ 10229570 inhibitor

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