A melanocortin receptor antagonist
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JNJ-10229570

Item No. 37768

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2,3-bis(2-methoxyphenyl)-1,2,4-thiadiazol-5(2H)-ylidene]-benzenamine
CAS Number
524923-88-4
Molecular Formula
C22H19N3O2S
Formula Weight
389.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
COC1=CC=CC=C1C(N(C2=CC=CC=C2OC)S3)=NC3=NC4=CC=CC=C4
InChi Code
InChI=1S/C22H19N3O2S/c1-26-19-14-8-6-12-17(19)21-24-22(23-16-10-4-3-5-11-16)28-25(21)18-13-7-9-15-20(18)27-2/h3-15H,1-2H3
InChi Key
XTHRTBCPBWJYRO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $61

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    5 mg

    $284

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    10 mg

    $447

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    25 mg

    $967

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    Product Description

    JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R), MC4R, and MC5R (IC50s = 270, 240, and 200 nM, respectively, in radioligand binding assays).1 It prevents bovine pituitary extract-induced increases in lipid droplets in primary human sebocytes when used at a concentration of 0.05 µM. JNJ-10229570 (1 µM) inhibits cholera toxin-induced increases in squalene and cholesterol esters, but not triglycerides, in primary human sebocytes. Topical application of JNJ-10229570 (0.05%) inhibits sebum secretion from, and sebaceous gland differentiation in, transplanted human skin in a mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Eisinger, M., Li, W.-H., Anthonavage, M., et al. A melanocortin receptor 1 and 5 antagonist inhibits sebaceous gland differentiation and the production of sebum-specific lipids. J. Dermatol. Sci. 63(1), 23-32 (2011).