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JNJ-10229570
CAS No. 524923-88-4
JNJ-10229570( JNJ10229570 | JNJ 10229570 )
Catalog No. M14856 CAS No. 524923-88-4
JNJ-10229570 (JNJ10229570) is a novel potent, selective melanocortin receptor MC1R and MC5R antagonist with binding IC50 of 270 nM and 200 nM, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 215 | In Stock |
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| 10MG | 335 | In Stock |
|
| 25MG | 566 | In Stock |
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| 50MG | 806 | In Stock |
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| 100MG | 1098 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameJNJ-10229570
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NoteResearch use only, not for human use.
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Brief DescriptionJNJ-10229570 (JNJ10229570) is a novel potent, selective melanocortin receptor MC1R and MC5R antagonist with binding IC50 of 270 nM and 200 nM, respectively.
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DescriptionJNJ-10229570 (JNJ10229570) is a novel potent, selective melanocortin receptor MC1R and MC5R antagonist with binding IC50 of 270 nM and 200 nM, respectively; dose dependently inhibited the production of sebaceous lipids in cultured primary human sebocytes; 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).Other Indication Phase 2 Discontinued.
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In VitroJNJ-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.
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In VivoTopical 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.
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SynonymsJNJ10229570 | JNJ 10229570
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PathwayGPCR/G Protein
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TargetMelanocortin Receptor
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RecptorMelanocortin Receptor
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Research AreaOther Indications
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IndicationOther Disease
Chemical Information
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CAS Number524923-88-4
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Formula Weight389.47
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Molecular FormulaC22H19N3O2S
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Purity>98% (HPLC)
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SolubilityDMSO : 62.5 mg/mL 160.47 mM
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SMILESCOC1=CC=CC=C1C2=N/C(SN2C3=CC=CC=C3OC)=N\C4=CC=CC=C4
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Chemical NameBenzenamine, N-(2,3-bis(2-methoxyphenyl)-1,2,4-thiadiazol-5(2H)-ylidene)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Eisinger M, et al. J Dermatol Sci. 2011 Jul;63(1):23-32. doi: 10.1016/j.jdermsci.2011.04.001.
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