SML0809

LE 135

≥98% (HPLC)

• Sinonimo/i: 4-(7,8,9,10-Tetrahydro-5,7,7,10,10-pentamethyl-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)-benzoic acid, LE-135
• Formula empirica (notazione di Hill): C₂₉H₃₀N₂O₂
• Numero CAS: 155877-83-1
• Peso molecolare: 438.56
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥98% (HPLC)
• Forma fisica: powder
• Colore: yellow to orange
• Solubilità: DMSO: 15 mg/mL, clear
• Temperatura di conservazione: 2-8°C
• InChI: 1S/C29H30N2O2/c1-28(2)14-15-29(3,4)22-17-25-23(16-21(22)28)30-26(18-10-12-19(13-11-18)27(32)33)20-8-6-7-9-24(20)31(25)5/h6-13,16-17H,14-15H2,1-5H3,(H,32,33); YZZAIQOVMHVWBS-UHFFFAOYSA-N

Descrizione

Applicazioni

LE 135 has been used for in vitro islet treatment.

Azioni biochim/fisiol

LE135 is a retinoic acid receptor (RAR) antagonist with selectivity for RARβ (Ki = 220 nM) over RARα (Ki = 1.4 μM). LE135 inhibits retinoic acid-induced transcriptional activation of RARβ (>70% inhibition at 10 μM), but not RARα, RARγ or retinoid X receptor α (RXRα). There is high interest in retinoic acid receptors for cancer and for differentiation studies. LE135 has been shown to inhibit retinoid Am80-induced differentiation of human promyelocytic leukemia HL-60 cells with an IC₅₀ value of 0.2 μM. LE135 has been used to study the role of a retinoic acid receptor-β (RARβ) on the differentiation of mesenchymal stem cells, and was found to inhibit the neuronal differentiation promoting effects of all-trans retinoic acid (ATRA) on mesenchymal stem cells.

Caratteristiche e vantaggi

This compound is featured on the Nuclear Receptors (Non-Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Informazioni sulla sicurezza

• Pittogrammi: GHS07
• Avvertenze: Warning
• Indicazioni di pericolo: H315,H319
• Consigli di prudenza: P264 - P280 - P302 + P352 - P305 + P351 + P338 - P332 + P313 - P337 + P313
• Classi di pericolo: Eye Irrit. 2 - Skin Irrit. 2
• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable