LE 135

Modify Date: 2024-01-06 19:30:28

LE 135 structure	Common Name	LE 135
	CAS Number	155877-83-1	Molecular Weight	438.561
	Density	1.2±0.1 g/cm3	Boiling Point	601.3±55.0 °C at 760 mmHg
	Molecular Formula	C₂₉H₃₀N₂O₂	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	317.5±31.5 °C
	Symbol	GHS07	Signal Word	Warning

Use of LE 135

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[1][2].

Name	4-(5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,4]benzodiazepin-13-yl)benzoic acid
Synonym	More Synonyms

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[1][2].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel Research Areas >> Cancer Research Areas >> Neurological Disease Signaling Pathways >> Metabolic Enzyme/Protease >> RAR/RXR
Target	RARβ:220 nM (Ki) RARα:1400 nM (Ki) TRPV1:2.5 μM (EC50) TRPA1:20 μM (EC50)
In Vitro	LE135 inhibits Am80-induced differentiation of human promyelocytic leukemia cells HL-60 with an IC50 of 150 nM[1]. LE135 inhibits retinoic acid (RA)-induced transcriptional activation of RARβ, but not RARα, RARγ or retinoid X receptor α (RXRα), on a variety of RA response elements. LE135 strongly represses 12-O-tetradecanoylphorbol-13-acetate-induced AP-1 activity in the presence of RARβ and RXRα[3].
In Vivo	LE135 provokes nociceptive responses and elicited thermal hyperalgesia mainly through TRPV1 channels, but required both TRPA1 and TRPV1 channels for producing mechanical allodynia. Intraplantar injection of LE135 (30 nmol/10 μL) induces mechanical hypersensitivity in wild-type and Trpa1−/− mice[2].
References	[1]. H Umemiya, et al. Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers. J Med Chem. 1997 Dec 19;40(26):4222-34. [2]. Shijin Yin, et al. LE135, a retinoid acid receptor antagonist, produces pain through direct activation of TRP channels. Br J Pharmacol. 2014 Mar;171(6):1510-20. [3]. Y Li, et al. Identification of a novel class of retinoic acid receptor beta-selective retinoid antagonists and their inhibitory effects on AP-1 activity and retinoic acid-induced apoptosis in human breast cancer cells. J Biol Chem. 1999 May 28;274(22):15360-6.

Density	1.2±0.1 g/cm3
Boiling Point	601.3±55.0 °C at 760 mmHg
Molecular Formula	C₂₉H₃₀N₂O₂
Molecular Weight	438.561
Flash Point	317.5±31.5 °C
Exact Mass	438.230713
PSA	52.90000
LogP	7.36
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.628
Storage condition	2-8°C

LE 135 MSDS(Chinese)

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H315-H319
Precautionary Statements	P305 + P351 + P338
Hazard Codes	Xi
RIDADR	NONH for all modes of transport

4-(5,7,7,10,10-Pentamethyl-7,8,9,10-tetrahydro-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)benzoic acid

hms3268h07

Benzoic acid, 4-(7,8,9,10-tetrahydro-5,7,7,10,10-pentamethyl-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)-

le 135

DC Chemicals Limited
China
Product Name: LE-135
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 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
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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LE 135

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