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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- CAS No.: 156691-86-0
- Formule: C23H28O2S
- Masse moléculaire:368.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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RXR α 11 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| HL-60 | EC50 |
5 nM
Compound: 6
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Transglutaminase activity in HL-60 cdm-1 cells
Transglutaminase activity in HL-60 cdm-1 cells
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[PMID: 7636843] |
AGN-191659 (Compound 6) acts as a pan-agonist in HeLa cells expressing chimeric retinoic acid receptors, and activates ER-RARβ (EC50 = 23 nM), ER-RARγ (EC50 = 37 nM) and ER-RXRα (EC50 = 11 nM)[1].
AGN-191659 (24 h) induces tissue-type transglutaminase activity in human promyelocytic leukemia cells HL-60 cdm-1, with an EC50 of 5 nM[1].
AGN-191659 (72 h) inhibits chondrogenesis in high-density micromass cultures of mouse embryonic limb bud cells on day 11, with an IC50 of 15 nM[1].
AGN-191659 binds to RXR α, RXR β, RXR γ, and RAR β, with corresponding Kd values of 120 nM, 139 nM, 214 nM, and 2700 nM[2].
AGN-191659 (0.001-10 μM; 24 h) inhibits bFGF-induced proliferation of passage 2-3 canine aortic endothelial cells via [3H]thymidine incorporation assay, with an IC50 of 50 nM[2].
AGN-191659 (0.001-10 μM; 48 h) dose-dependently inhibits the bFGF-induced increase in cell number in growth-arrested canine aortic endothelial cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Passage 2-3 canine aortic endothelial cells
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Concentration:0.001-10 μM
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Incubation Time:24 h (total, co-incubated with 10 ng/mL bFGF)
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Result:Inhibited bFGF-induced [3H]thymidine incorporation with an IC50 of 50 nM.
Reduced incorporation to near 10% of bFGF-stimulated control levels at 10 μM.
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Cell Line:Growth-arrested canine aortic endothelial cells
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Concentration:0.001-10 μM
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Incubation Time:48 h (co-incubated with 10 ng/mL bFGF)
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Result:Dose-dependently reduced bFGF-induced increases in cell number.
Reduced cell number to ~5000 cells (from ~30,000 in bFGF-only controls) at 10 μM.
AGN-191659 (10-250 μmol/kg; p.o.; daily; for 3 consecutive days) dose-dependently induces severe hypertriglyceridemia in male Fischer rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CDF (F-344)/CrlBR (male, 6-7 weeks old)[3]
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Dosage:10 μmol/kg; 30 μmol/kg; 100 μmol/kg; 250 μmol/kg; 20 μmol/kg
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Administration:p.o.; daily; 3 consecutive days
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Result:Induced a 6-fold elevation in serum triglycerides (mean ~290 mg/dL, significantly different from vehicle control).
Induced an ~8-fold elevation in serum triglycerides (mean ~400 mg/dL, significantly different from vehicle control).
Induced an ~9-fold elevation in serum triglycerides (mean ~460 mg/dL, significantly different from vehicle control) with 13% weight loss in treated rats.
Induced an ~9-fold elevation in serum triglycerides (mean ~480 mg/dL, significantly different from vehicle control) with 23% weight loss in treated rats.
Reduced plasma post-heparin lipolytic activity by 89% (mean 4.7 nmol/min/mL, significantly different from vehicle control) and increased serum triglycerides to a mean of 589 mg/dL (significantly different from vehicle control).
Chemical Information
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CAS No. 156691-86-0
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Masse moléculaire 368.54
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Formule C23H28O2S
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SMILES
CC1(C)C=2C(C(C)(C)CC1)=CC(C)=C(\C(=C\C=3SC(C(O)=O)=CC3)\C)C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AGN-191659 Related Classifications
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