LE135

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

LE135 inhibits Am80-induced differentiation of human promyelocytic leukemia cells HL-60 with an IC50 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.

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Metabolic Enzyme/Protease

Retinoid Receptor

Retinoid Receptor

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155877-83-1

438.56

C29H30N2O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (114.01 mM; 超声助溶 )

CN1c2cc3c(cc2N=C(c2ccc(cc2)C(O)=O)c2ccccc12)C(C)(C)CCC3(C)C

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(-20℃)

With Ice Pack

≥ 2 years