524923-88-4

524923-88-4 structure

Name: JNJ-10229570
Chemical Name: 2,3-bis(2-methoxyphenyl)-N-phenyl-1,2,4-thiadiazol-5-imine
CAS Number: 524923-88-4
Molecular Formula: C₂₂H₁₉N₃O₂S
Molecular Weight: 389.47000
Catalog: Research Areas Others
Create Date: 2017-06-23 05:48:25
Modify Date: 2024-01-12 11:13:47
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.

Name	2,3-bis(2-methoxyphenyl)-N-phenyl-1,2,4-thiadiazol-5-imine
Synonyms	unii-n9ix402l35 JNJ-10229570

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. 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.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Melanocortin Receptor Research Areas >> Others
Target	IC50: 270 nM (human MC1R), 200 nM (human MC5R)[1].
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[1].
In Vivo	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[1].
Animal Admin	Mice[1] Human skins transplanted onto SCID mice are topically treated with vehicle or JNJ-10229570 (0.05%) for 30 days[1].
References	[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.

Molecular Formula	C₂₂H₁₉N₃O₂S
Molecular Weight	389.47000
Exact Mass	389.12000
PSA	76.88000
LogP	4.85040
Storage condition	-20℃

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