Product Details
| Product Name:
LE135 |
CAS No.:
155877-83-1 |
| Purity:
98.33% |
Supply Ability:
10g |
| Release date:
2026/04/21 |
Product Introduction
Bioactivity
| Name | LE135 |
| 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. |
| 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.56 mM), Sonication is recommended.
DMSO : 25 mg/mL (57 mM), Sonication is recommended.
|
| Keywords | RetinoidReceptor | Retinoid Receptor | RARβ | LE-135 | LE135 |
| Inhibitors Related | Isotretinoin | 1,3,5-Triisopropylbenzene | (+)-Camphor | Rosiglitazone | Caffeic Acid | Retinoic acid | Camphor | Probenecid | 1,4-Cineole | 2,4-Di-tert-butylphenol | trans-Cinnamaldehyde | Magnolol |
| Related Compound Libraries | Bioactive Compound Library | Cancer Cell Differentiation Compound Library | Inhibitor Library | Metabolism Compound Library | Bioactive Compounds Library Max | Neuronal Differentiation Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States