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LE135
🥰Excellent
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
🥰Excellent
Purity: 98.33%
Catalog No. T22920Alias LE 135Cas No. 155877-83-1
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $39 | In Stock | |
| 2 mg | $56 | In Stock | |
| 5 mg | $93 | In Stock | |
| 10 mg | $137 | In Stock | |
| 25 mg | $229 | In Stock | |
| 50 mg | $342 | In Stock | |
| 100 mg | $497 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $98 | In Stock |
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Purity:98.33%
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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.Product Introduction
Bioactivity
Chemical Properties
| 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 | RARβ:220 nM (Ki), TRPV1:2.5 μM (EC50), TRPA1:20 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]. |
| Alias | LE 135 |
| 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. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45 mg/mL (102.6 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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