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[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].

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].

155877-83-1

C29H30N2O2

438.56

LE 135

DMSO:45mg/mL (102.6mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years