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LE135
$115 – $127
Products Details
Product Description
– 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[1][2].
Web ID
– HY-107436
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C29H30N2O2
References
– [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.
CAS Number
– 155877-83-1
Molecular Weight
– 438.56
Compound Purity
– 99.03
SMILES
– O=C(O)C1=CC=C(C2=NC3=CC4=C(C(C)(C)CCC4(C)C)C=C3N(C)C5=CC=CC=C52)C=C1
Clinical Information
– No Development Reported
Research Area
– Cancer; Neurological Disease
Solubility
– DMSO : 50 mg/mL (ultrasonic)
Target
– RAR/RXR;TRP Channel
Isoform
– TRPA;TRPV
Pathway
– Membrane Transporter/Ion Channel;Metabolic Enzyme/Protease;Neuronal Signaling;Vitamin D Related/Nuclear Receptor
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
