1. Metabolic Enzyme/Protease
    Neuronal Signaling
    Membrane Transporter/Ion Channel
  2. RAR/RXR
    TRP Channel
  3. LE135

LE135 

Cat. No.: HY-107436 Purity: 98.13%
Handling Instructions

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.

For research use only. We do not sell to patients.

LE135 Chemical Structure

LE135 Chemical Structure

CAS No. : 155877-83-1

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Estimated Time of Arrival: December 31
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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].

IC50 & Target[1][2]

RARβ

220 nM (Ki)

RARα

1400 nM (Ki)

TRPV1

2.5 μM (EC50)

TRPA1

20 μM (EC50)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

438.56

Formula

C₂₉H₃₀N₂O₂

CAS No.

155877-83-1

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References

Purity: 98.13%

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Keywords:

LE135LE 135LE-135RAR/RXRTRP ChannelRetinoic acid receptorsRetinoid X receptorsTransient receptor potential channelsRARβRARαdiazepinylbenzoicAP-1retinoidTRPV1TRPA1Inhibitorinhibitorinhibit

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LE135
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HY-107436
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