156691-86-0
Chemical Structure
AGN-191659
- CAS No.: 156691-86-0
- Formula:C23H28O2S
- Molecular Weight:368.54
IUPAC Name: (E)-5-(2-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-1-en-1-yl)thiophene-2-carboxylic acid
InChIKey: QPAMXNZWXFZISY-SDNWHVSQSA-N
SMILES: CC1(C)C=2C(C(C)(C)CC1)=CC(C)=C(\C(=C\C=3SC(C(O)=O)=CC3)\C)C2
Biological Activity: AGN-191659 is an orally active RAR/RXR agonist with EC50 values of 11 nM, 23 nM, and 37 nM for RXRα, RARβ, and RARγ, respectively. AGN-191659 activates RXRα, RARβ and RARγ to induce gene transcription. AGN-191659 induces tissue transglutaminase activity, inhibits ornithine decarboxylase activity induced by tumor promoters, and suppresses chondrogenesis. AGN-191659 reverses basic fibroblast growth factor-induced endothelial cell proliferation. AGN-191659 induces hypertriglyceridemia in rat models. AGN-191659 inhibits total heparin-releasable lipase activity. AGN-191659 can be used in research related to promyelocytic leukemia and hypertriglyceridemia[1][2][3].
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AGN-191659 | AGN-191659 is an orally active RAR/RXR agonist with EC50 values of 11 nM, 23 nM, and 37 nM for RXRα, RARβ, and RARγ, respectively. AGN-191659 activates RXRα, RARβ and RARγ to induce gene transcription. AGN-191659 induces tissue transglutaminase activity, inhibits ornithine decarboxylase activity induced by tumor promoters, and suppresses chondrogenesis. AGN-191659 reverses basic fibroblast growth factor-induced endothelial cell proliferation. AGN-191659 induces hypertriglyceridemia in rat models. AGN-191659 inhibits total heparin-releasable lipase activity. AGN-191659 can be used in research related to promyelocytic leukemia and hypertriglyceridemia. | |||||||||||||||||||||
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References
- [1]. Beard RL, et al. Synthesis and structure-activity relationships of stilbene retinoid analogs substituted with heteroaromatic carboxylic acids. J Med Chem. 1995;38(15):2820-2829. [Content Brief]
- [2]. Pakala R, et al. Modulation of endothelial cell proliferation by retinoid x receptor agonists. Eur J Pharmacol. 1999;385(2-3):255-261. [Content Brief]
- [3]. Standeven AM, et al. Retinoid X receptor agonist elevation of serum triglycerides in rats by potentiation of retinoic acid receptor agonist induction or by action as single agents. Biochem Pharmacol. 2001;62(11):1501-1509. [Content Brief]
