JNJ-10229570

SKU: orb1301769

Description

JNJ-10229570

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 524923-88-4
• MW: 389.47
• Purity: 99.06%
• Formula: C₂₂H₁₉N₃O₂S
• SMILES: COc1ccccc1-c1n\c(=N\c2ccccc2)sn1-c1ccccc1OC
• Target: Melanocortin Receptor
• Solubility: DMSO:62.5 mg/mL (160.47 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.14 mM)

Bioactivity

• Target IC50:
  MC5R (human):200 nM|MC1R (human):270 nM
• In Vivo:
  Topical treatment with JNJ-10229570 on human skins transplanted onto SCID mice significantly reduced sebum-specific lipid production, sebaceous gland size, and the expression of the sebaceous differentiation marker epithelial-membrane antigen (EMA). Treatment with flutamide, a known inhibitor of sebum production, validates the human skin/SCID mouse experimental system for sebaceous secretion studies.
• In Vitro:
  JNJ-10229570 demonstrates dose-dependent inhibition of sebaceous lipid production in cultured primary human sebocytes. Concurrently, JNJ-7818369 effectively prevents the attachment of 125I-NDP-α-MSH to cells featuring human MC1R and MC5R receptors, presenting IC50 values of 270±120 nM and 200±50 nM, respectively. Similar efficacy is observed with the compound's free base form. For both variations of the compound, the inhibitory action on MC4R is identical, with IC50 values reported at 240±170 nM. Notably, treatment with JNJ-10229570 at a concentration of 0.01 μM markedly suppresses lipid granule formation, achieving total inhibition at a concentration of 0.05 μM.
• Cell Research:
  Radioligand binding assays were performed, with CHO-K1 cells over-expressing MC1R, and HEK-293 cells over-expressing MC4R or MC5R, using a single concentration of 125I-NDP-a-MSH and increasing concentrations of JNJ-7818369 or JNJ-10229570. IC50 values for inhibition of radioligand binding were calculated by a non-linear, least squares regression method.
• Animal Research:
  JNJ-10229570 (0.05%) and flutamide (5%) were dissolved in a vehicle of ethanol: propylene glycol (7:3). 20 ml/1.5 cm^2 were applied onto each skin xenograft, starting at three months posttransplantation. Xenografts were treated once daily, 5 days/week, for 30 34 treatments. Xenografts were then collected for histological examination and lipid analysis. Each study was repeated with skin xenografts from at least 3 donors. The vehicle had no effect on sebaceous glands differentiation or activity.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, Melanocortin Receptor, melanocortin-1 receptor, melanocortin-5 receptor (MC5R), MelanocortinReceptor, MC Receptor, inhibit, JNJ 10229570, JNJ10229570, JNJ-10229570, UNII-N9IX402L35

Compound Identifiers

PubChem CID

10110895