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LE135

Name: LE135
Brand: TargetMol
SKU: T22920
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T22920Cas No. 155877-83-1

Alias LE 135

LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), showing higher affinity for RARβ. It is highly selective over RARγ, RXRα, RXRβ, and RXRγ. LE135 also acts as a potent TRPV1 and TRPA1 receptor activator with EC50s of 2.5 μM and 20 μM, respectively.

LE135

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Purity: 97.94%

Catalog No. T22920Alias LE 135Cas No. 155877-83-1

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$39	In Stock	In Stock
2 mg	$56	In Stock	In Stock
5 mg	$93	In Stock	In Stock
10 mg	$137	In Stock	In Stock
25 mg	$229	In Stock	In Stock
50 mg	$342	In Stock	In Stock
100 mg	$497	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$98	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:97.94%

Appearance:Solid

Color:Orange

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), showing higher affinity for RARβ. It is highly selective over RARγ, RXRα, RXRβ, and RXRγ. LE135 also acts as a potent TRPV1 and TRPA1 receptor activator with EC50s of 2.5 μM and 20 μM, respectively.
Targets&IC50	TRPA1:20 μM (EC50), RARβ:220 nM (Ki), TRPV1:2.5 μM (EC50), RARα:1400 nM (Ki)
In vitro	LE135 blocks the differentiation of human promyelocytic leukemia cells HL-60, triggered by Am80, with an inhibitory concentration (IC50) of 150 nM. It specifically hinders retinoic acid (RA)-prompted transcriptional activation of the retinoic acid receptor beta (RARβ) without affecting RARα, RARγ, or the retinoid X receptor alpha (RXRα) across various RA response elements. Furthermore, LE135 significantly suppresses the activity of the AP-1 transcription factor induced by 12-O-tetradecanoylphorbol-13-acetate in cells that express RARβ and RXRα.
In vivo	LE135 induces nociceptive responses and thermal hyperalgesia primarily via TRPV1 channels, and necessitates both TRPA1 and TRPV1 channels to cause mechanical allodynia. Intraplantar injection of LE135 (30 nmol/10 μL) results in mechanical hypersensitivity in both wild-type and Trpa1−/− mice[2].
Synonyms	LE 135

Chemical Properties

Molecular Weight	438.56
Formula	C₂₉H₃₀N₂O₂
Cas No.	155877-83-1
Smiles	CN1c2cc3c(cc2N=C(c2ccc(cc2)C(O)=O)c2ccccc12)C(C)(C)CCC3(C)C
Relative Density.	1.17 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 25 mg/mL (57 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.56 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2802 mL	11.4009 mL	22.8019 mL	114.0095 mL
5 mM	0.4560 mL	2.2802 mL	4.5604 mL	22.8019 mL
10 mM	0.2280 mL	1.1401 mL	2.2802 mL	11.4009 mL
20 mM	0.1140 mL	0.5700 mL	1.1401 mL	5.7005 mL
50 mM	0.0456 mL	0.2280 mL	0.4560 mL	2.2802 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc