LE135
产品说明书
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同义名 : | - |
| CAS号 : | 155877-83-1 | |
| 货号 : | A405975 | |
| 分子式 : | C29H30N2O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 438.56 | |
| MDL号 : | MFCD06798318 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | LE135 is a potent RAR antagonist that selectively binds to RARα/RARβ with Ki values of 1.4 μM and 220 nM, respectively, and has a higher affinity for RARβ. LE135 is highly selective for RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent activator of TRPV1 and TRPA1 receptors with EC50s of 2.5 μM and 20 μM, respectively [1][2].LE135 inhibits Am80-induced differentiation of human promyelocytic leukaemia cells HL-60 with an IC50 of 150 nM[1].LE135 inhibits retinoic acid (RA)-induced transcriptional activation of RARβ, but not RARα, RARγ, or RXRα on a variety of RA response elements. In the presence of RARβ and RXRα, LE135 strongly inhibits 12-O-tetradecanoylphorbol-13-acetate-induced AP-1 activity[3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.28mL 0.46mL 0.23mL |
11.40mL 2.28mL 1.14mL |
22.80mL 4.56mL 2.28mL |
