JNJ-10229570 NEW
| Price | $112 | $198 | $313 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: JNJ-10229570 | CAS No.: 524923-88-4 |
| Purity: 99.06% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | JNJ-10229570 |
| 描述 | JNJ-10229570 (UNII-N9IX402L35) 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. |
| 細(xì)胞實(shí)驗(yàn) | 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. |
| 動(dòng)物實(shí)驗(yàn) | 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. |
| 體外活性 | 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. |
| 體內(nèi)活性 | 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. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 62.5 mg/mL (160.47 mM) |
| 關(guān)鍵字 | MC Receptor | Inhibitor | JNJ-10229570 | inhibit | Melanocortin Receptor |
| 相關(guān)產(chǎn)品 | HS 014 acetate(207678-81-7 free base) | MCL0020 | Beta-MSH (1-22) (human) acetate | ACTH (1-17) acetate | Neuropeptide EI, rat acetate | [D-Trp8]-γ-MSH acetate(321351-81-9 free base) | a-MSH, amide Acetate(581-05-5 free base) | Undecylenoyl phenylalanine | ACTH 11-24 acetate(4237-93-8 free base) | Melanotan (MT)-II | HS024 | Nonapeptide-1 acetate salt (158563-45-2 free base) |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 神經(jīng)信號(hào)分子庫 | 膜蛋白靶向化合物庫 | 抗肥胖化合物庫 | 抑制劑庫 | NO PAINS 化合物庫 | 已知活性化合物庫 | GPCR靶點(diǎn)分子庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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