Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LE135 是一种有效的 RAR 拮抗剂,可选择性结合 RARα (Ki 为 1.4 μM) 和 RARβ (Ki 为 220 nM),对 RARβ 具有更高的亲和力。LE135 对 RARγ,RXRα,RXRβ 和 RXRγ 具有高度选择性。LE135 还是一种有效的 TRPV1 和 TRPA1 受体激活剂,EC50 分别为 2.5 μM 和 20 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 395 | 现货 | ||
2 mg | ¥ 573 | 现货 | ||
5 mg | ¥ 980 | 现货 | ||
10 mg | ¥ 1,470 | 现货 | ||
25 mg | ¥ 2,490 | 现货 | ||
50 mg | ¥ 3,670 | 现货 | ||
100 mg | ¥ 5,230 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,090 | 现货 |
产品描述 | LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5 μM and 20 μM, respectively. |
靶点活性 | RARβ:220 nM (Ki), TRPV1:2.5 μM (EC50), TRPA1:20 μM (EC50), RARα:1400 nM (Ki) |
体外活性 | LE135 inhibits Am80-induced differentiation of human promyelocytic leukemia 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 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[3]. |
体内活性 | 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[2]. |
别名 | LE 135 |
分子量 | 438.56 |
分子式 | C29H30N2O2 |
CAS No. | 155877-83-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (102.6 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2802 mL | 11.4009 mL | 22.8019 mL | 57.0047 mL |
5 mM | 0.456 mL | 2.2802 mL | 4.5604 mL | 11.4009 mL | |
10 mM | 0.228 mL | 1.1401 mL | 2.2802 mL | 5.7005 mL | |
20 mM | 0.114 mL | 0.57 mL | 1.1401 mL | 2.8502 mL | |
50 mM | 0.0456 mL | 0.228 mL | 0.456 mL | 1.1401 mL | |
100 mM | 0.0228 mL | 0.114 mL | 0.228 mL | 0.57 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
LE135 155877-83-1 Metabolism Retinoid Receptor LE-135 LE 135 Inhibitor inhibitor inhibit