Product 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), 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.
CAS:
155877-83-1
Molecular Weight:
438.56
Formula:
C29H30N2O2
Chemical Name:
4-2,14,14,17,17-pentamethyl-2,10-diazatetracyclo[9.8.0.0³,⁸.0¹³,¹⁸]nonadeca-1(19),3,5,7,9,11,13(18)-heptaen-9-ylbenzoic acid
Smiles :
CC1(C)CCC(C)(C)C2C=C3N=C(C4=CC=CC=C4N(C)C3=CC1=2)C1C=CC(=CC=1)C(O)=O
InChiKey:
YZZAIQOVMHVWBS-UHFFFAOYSA-N
InChi :
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)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.|Product information|CAS Number: 155877-83-1|Molecular Weight: 438.56|Formula: C29H30N2O2|Chemical Name: 4-2,14,14,17,17-pentamethyl-2,10-diazatetracyclo[9.8.0.0³,⁸.0¹³,¹⁸]nonadeca-1(19),3,5,7,9,11,13(18)-heptaen-9-ylbenzoic acid|Smiles: CC1(C)CCC(C)(C)C2C=C3N=C(C4=CC=CC=C4N(C)C3=CC1=2)C1C=CC(=CC=1)C(O)=O|InChiKey: YZZAIQOVMHVWBS-UHFFFAOYSA-N|InChi: 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)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Telitacicept Formula |Shelf Life: ≥12 months if stored properly.Bethanechol Cancer |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:32644631 |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|LE135 inhibits Am80-induced differentiation of human promyelocytic leukemia cells HL-60 with an IC50 of 150 nM. 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.|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.|References:|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.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.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.Products are for research use only. Not for human use.|
