188844-52-2

Basic information

• Product Name: HX 630
• Synonyms: HX 630;4-(7,8,9,10-tetrahydro-7,7,10,10-tetraMethylbenzo[b]naphtho[2,3-f][1,4]thiazepin-12-yl)benzoic Acid
• CAS NO: 188844-52-2
• Molecular Formula: C28H27NO2S
• Molecular Weight: 441.58448
• Product Categories: Agonist;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;Agonist, Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals, Sulfur & Selenium Compounds
• Mol File: 188844-52-2.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• CAS DataBase Reference: HX 630(CAS DataBase Reference)
• NIST Chemistry Reference: HX 630(188844-52-2)
• EPA Substance Registry System: HX 630(188844-52-2)

Safety Data

• Hazardous Substances Data: 188844-52-2(Hazardous Substances Data)

Usage

Uses

A nuclear receptor retinoid X receptor (RXR) agonist that exerts antiproliferative effects in vascular smooth muscle cells (VSMCs) in vivo and in vitro. A potential therapeutic target for vascular injury and intimal thickening. It efficiently enhanced ABCA1 mRNA expression and apoA-I-dependent cellular cholesterol release in differentiated THP-1 cells.

Upstream product

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• 188845-37-6 N-[2-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-ylsulfanyl)-phenyl]-terephthalamic acid methyl ester 
• 132392-27-9 5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-thiol 
• 88-73-3 2-Chloronitrobenzene 
• 7377-26-6 4-Methoxycarbonylbenzoyl chloride 
• 188845-38-7 4-(7,7,10,10-Tetramethyl-7,8,9,10-tetrahydro-5-thia-13-aza-benzo[4,5]cyclohepta[1,2-b]naphthalen-12-yl)-benzoic acid methyl ester 
• 188845-36-5 s-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphtalenyl)-2-aminothiophenol 

Relevant articles and documents

Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers

In human HL-60 promyelocytic leukemia cells, diazepinylbenzoic acid derivatives can exhibit either antagonistic or synergistic effects on the differentiation-inducing activities of natural or synthetic retinoids, the activity depending largely on the nature of the substituents on the diazepine ring. Thus, a benzolog of the retinoid antagonist LE135 (6), 4-(13H- 10,11,12,13-tetrahydro-10,10,13,13,15-pentamethyldinaphtho[2,3-b][1,2- e]diazepin-7-yl)benzoic acid (LE540, 17), exhibits a 1 order of magnitude higher antagonistic potential than the parental LE135 (6). In contrast, 4- [5H-2,3-(2,5-dimethyl-2,5-hexano)-5-methyldibenzo[b,e][1,4]diazepin-11-yl]- benzoic acid (HX600, 7), a structural isomer of the antagonistic LE135 (6), enhanced HL-60 cell differentiation induced by RAR agonists, such as Am80 (2). This synergistic effect was further increased for a thiazepine, HX630 (29), and an azepine derivative, HX640 (30); both synergized with Am80 (2) more potently than HX600 (7). Notably, the negative and positive effects of the azepine derivatives on retinoidal actions can be related to their RAR- antagonistic and RXR-agonistic properties, respectively, in the context of the RAR-RXR heterodimer.