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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 156691-86-0
- Formel: C23H28O2S
- Molecular Weight:368.54
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
|
RXR α 11 nM (EC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | EC50 |
5 nM
Compound: 6
|
Transglutaminase activity in HL-60 cdm-1 cells
Transglutaminase activity in HL-60 cdm-1 cells
|
[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.
-
Cell Line:Passage 2-3 canine aortic endothelial cells
-
Concentration:0.001-10 μM
-
Incubation Time:24 h (total, co-incubated with 10 ng/mL bFGF)
-
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.
-
Cell Line:Growth-arrested canine aortic endothelial cells
-
Concentration:0.001-10 μM
-
Incubation Time:48 h (co-incubated with 10 ng/mL bFGF)
-
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.
-
Animal Model:CDF (F-344)/CrlBR (male, 6-7 weeks old)[3]
-
Dosage:10 μmol/kg; 30 μmol/kg; 100 μmol/kg; 250 μmol/kg; 20 μmol/kg
-
Administration:p.o.; daily; 3 consecutive days
-
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
-
CAS. Nr. 156691-86-0
-
Molecular Weight 368.54
-
Formel C23H28O2S
-
SMILES
CC1(C)C=2C(C(C)(C)CC1)=CC(C)=C(\C(=C\C=3SC(C(O)=O)=CC3)\C)C2
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AGN-191659 Related Classifications
HY-167262 Related Classifications
Powered by Bioz