LE 135
| 中文名称 | LE 135 |
|---|---|
| 中文同义词 | 化合物 T22920;化合物LE135;4-(5,7,7,10,10-五甲基-7,8,9,10-四氢-5H-苯并[E]萘并[2,3-B][1,4]二氮杂卓-13-基)苯甲酸;LE 135,RARΒ拮抗剂;化合物LE135,10 MM DMSO 溶液 |
| 英文名称 | 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 |
| 英文同义词 | LE 135;4-(7,8,9,10-Tetrahydro-5,7,7,10,10-pentamethyl-(5H)-benzo[e]naphtho[2.3-b][1.4]diazepine-13-yl)benzoicacid;Benzoic acid, 4-(7,8,9,10-tetrahydro-5,7,7,10,10-pentaMethyl-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)-;4-(5,7,7,10,10-Pentamethyl-7,8,9,10-tetrahydro-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)benzoic acid;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;LE135, 10 mM in DMSO |
| CAS号 | 155877-83-1 |
| 分子式 | C29H30N2O2 |
| 分子量 | 438.56 |
| EINECS号 | |
| 相关类别 | Intracellular receptor |
| Mol文件 | 155877-83-1.mol |
| 结构式 |  |
LE 135 性质
| 沸点 | 601.3±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.17±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | DMSO：可溶15mg/mL，澄清 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 3.02±0.10(Predicted) |
| 颜色 | 黄色至橙色粘性至蜡状 |
| 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) |
| InChIKey | YZZAIQOVMHVWBS-UHFFFAOYSA-N |
| SMILES | N1(c2c(cc5c(c2)C(CCC5(C)C)(C)C)N=C(c4c1cccc4)c3ccc(cc3)C(=O)O)C |
|
RARβ 220 nM (Ki) |
RARα 1400 nM (Ki) |
TRPV1 2.5 μM (EC 50 ) |
TRPA1 20 μM (EC 50 ) |
LE135 inhibits Am80-induced differentiation of human promyelocytic leukemia cells HL-60 with an IC
50
of 150 nM.
LE135 inhibits retinoic acid (RA)-induced transcriptional activation of RARβ, but not RARα, RARγ or retinoid X receptor α (RXRα), on a variety of RA response elements. LE135 strongly represses 12-O-tetradecanoylphorbol-13-acetate-induced AP-1 activity in the presence of RARβ and RXRα.
LE135 provokes nociceptive responses and elicited thermal hyperalgesia mainly through TRPV1 channels, but required both TRPA1 and TRPV1 channels for producing mechanical allodynia. Intraplantar injection of LE135 (30 nmol/10 μL) induces mechanical hypersensitivity in wild-type and Trpa1 −/− mice.
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-107436 | LE135 | 155877-83-1 | 1 mg | 480元 |
| 2025/12/22 | HY-107436 | LE 135 LE135 | 155877-83-1 | 5mg | 997元 |