SML0809

LE 135

≥98% (HPLC)

• 别名: 4-(7,8,9,10-Tetrahydro-5,7,7,10,10-pentamethyl-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)-benzoic acid, LE-135
• 经验公式（希尔记法）: C₂₉H₃₀N₂O₂
• CAS号: 155877-83-1
• 分子量: 438.56
• UNSPSC代码: 12352200
• NACRES: NA.77

属性

• 质量水平: 100
• 方案: ≥98% (HPLC)
• 表单: powder
• 颜色: yellow to orange
• 溶解性: DMSO: 15 mg/mL, clear
• 储存温度: 2-8°C
• SMILES字符串: N1(c2c(cc5c(c2)C(CCC5(C)C)(C)C)N=C(c4c1cccc4)c3ccc(cc3)C(=O)O)C
• InChI: 1S/C29H30N2O2/c1-28(2)14-15-29(3,4)22-17-25-23(16-21(22)28)30-26(18-10-12-19(13-11-18)27(32)33)20-8-6-7-9-24(20)31(25)5/h6-13,16-17H,14-15H2,1-5H3,(H,32,33)
• InChI key: YZZAIQOVMHVWBS-UHFFFAOYSA-N

说明

应用

LE 135 has been used for in vitro islet treatment.

生化/生理作用

LE135 is a retinoic acid receptor (RAR) antagonist with selectivity for RARβ (Ki = 220 nM) over RARα (Ki = 1.4 μM).

LE135 is a retinoic acid receptor (RAR) antagonist with selectivity for RARβ (Ki = 220 nM) over RARα (Ki = 1.4 μM). LE135 inhibits retinoic acid-induced transcriptional activation of RARβ (>70% inhibition at 10 μM), but not RARα, RARγ or retinoid X receptor α (RXRα). There is high interest in retinoic acid receptors for cancer and for differentiation studies. LE135 has been shown to inhibit retinoid Am80-induced differentiation of human promyelocytic leukemia HL-60 cells with an IC₅₀ value of 0.2 μM. LE135 has been used to study the role of a retinoic acid receptor-β (RARβ) on the differentiation of mesenchymal stem cells, and was found to inhibit the neuronal differentiation promoting effects of all-trans retinoic acid (ATRA) on mesenchymal stem cells.

特点和优势

This compound is featured on the Nuclear Receptors (Non-Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

安全信息

• 象形图: GHS07
• 警示用语：: Warning
• 危险声明: H315,H319
• 预防措施声明: P264 - P280 - P302 + P352 - P305 + P351 + P338 - P332 + P313 - P337 + P313
• 危险分类: Eye Irrit. 2 - Skin Irrit. 2
• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 3
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable