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LE135

CAT: 0804-HY-107436-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-107436-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
155877-83-1
UNSPSC
12352005
Hazard Statement
H315, H319
Target
RAR/RXR; TRP Channel
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling; Vitamin D Related/Nuclear Receptor
Applications
Cancer-programmed cell death
Field of Research
Cancer; Neurological Disease
Assay Protocol
https://www.medchemexpress.com/le135.html
Concentration
10mM
Purity
99.0
Solubility
DMSO : 50 mg/mL (ultrasonic)
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
Molecular Formula
C29H30N2O2
Molecular Weight
438.56
Precautions
H315, H319
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
TRPA1; TRPV1

Alternative Products

CatalogName
T22920-01LE135

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