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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 |
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| 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
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Undecylenoyl phenyla...
Undecylenoyl phenylalanine is a novel depigmenting agent, which possibly acts as an alpha-melanocyte-stimulating hormone antagonist, thus inhibiting melaninogenesis.
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HS 024
Highly potent melanocortin MC4 receptor antagonist (Ki values are 0.29, 18.6, 5.45 and 3.29 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake, and blocks α-MSH- and MTII-induced hypotension and bradycardia in rats, following central administration in vivo.
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MSG 606
Potent human MC1 receptor antagonist (IC50 = 17 nM). Also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). Exhibits binding affinity for A375 melanoma cells in vitro. Reverses morphine-induced hyperalgesia in female mice, with no effect in male mice. γMSH analog.
