Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 39.00 | |
2 mg | In stock | $ 56.00 | |
5 mg | In stock | $ 93.00 | |
10 mg | In stock | $ 137.00 | |
25 mg | In stock | $ 229.00 | |
50 mg | In stock | $ 342.00 | |
100 mg | In stock | $ 497.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 98.00 |
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. |
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]. |
Synonyms | LE 135 |
Molecular Weight | 438.56 |
Formula | C29H30N2O2 |
CAS No. | 155877-83-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (102.6 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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LE135 155877-83-1 Metabolism Retinoid Receptor LE-135 LE 135 inhibitor inhibit