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.
Product information
CAS Number: 524923-88-4
Molecular Weight: 389.47
Formula: C22H19N3O2S
Chemical Name: (5Z)-2,3-bis(2-methoxyphenyl)-N-phenyl-2,5-dihydro-1,2,4-thiadiazol-5-imine
Smiles: COC1C=CC=CC=1N1S/C(/N=C1C1C=CC=CC=1OC)=N\C1C=CC=CC=1
InChiKey: XTHRTBCPBWJYRO-FCQUAONHSA-N
InChi: 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/b23-22-
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 62.5 mg/mL (160.47 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.