LE 135

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.


Cat. No.: EX-A6728	Purity: >98%

	Chemical structure of LE 135

For research only, Do not use for Human!

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CAS No.	155877-83-1
Purity	>98%
Formula	C29H30N2O2
Mol Weight	438.5607
Color	Yellow to brown
State	solid powder
Solubility	Soluble in DMSO 50 mg/mL
Shelf Life	>3 years if stored properly
Storage	Powder -20℃ 3 years, 4°C 2 years; In solvent -20℃ 1 month;
Shipping	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Reference:	[1]. H Umemiya, et al. Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers. J Med Chem. 1997 Dec 19;40(26):4222-34. [2]. Shijin Yin, et al. LE135, a retinoid acid receptor antagonist, produces pain through direct activation of TRP channels. Br J Pharmacol. 2014 Mar;171(6):1510-20. [3]. Y Li, et al. Identification of a novel class of retinoic acid receptor beta-selective retinoid antagonists and their inhibitory effects on AP-1 activity and retinoic acid-induced apoptosis in human breast cancer cells. J Biol Chem. 1999 May 28;274(22):15360-6.
CoA	CoA of LE 135


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