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JNJ-10229570

Catalog No. T5464 CAS 524923-88-4

Synonyms: JNJ10229570, JNJ 10229570, UNII-N9IX402L35

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

JNJ-10229570, CAS 524923-88-4

Pack Size	Availability	Price/USD
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

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Purity: 99.06%

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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

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 62.5 mg/mL (160.47 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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：

Inhibitor Library NO PAINS Compound Library Bioactive Compounds Library Max GPCR Compound Library Bioactive Compound Library Neuronal Signaling Compound Library

Related Products

Related compounds with same targets

HS 014 acetate(207678-81-7 free base) HS024 [D-Trp8]-γ-MSH acetate(321351-81-9 free base) Melanotan (MT)-II ACTH 11-24 acetate(4237-93-8 free base) α-MSH Adrenocorticotropic Hormone (ACTH) (4-10), human Bremelanotide Acetate

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Keywords

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

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