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