2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. RAR/RXR
  4. 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.

For research use only. We do not sell to patients.

AGN-191659

AGN-191659 Chemical Structure

CAS No. : 156691-86-0

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AGN-191659 Related Antibodies

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Description

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].

IC50 & Target[1]

RXR α

11 nM (EC50)

In Vitro

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.

AGN-191659 Related Antibodies

Cell Proliferation Assay[2]

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 Proliferation Assay[2]

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.
In Vivo

AGN-191659 (administered topically; 1 h prior to TPA treatment) inhibits 12-O-tetradecanoylphorbol-13-acetate (TPA, HY-18739)-induced ornithine decarboxylase (ODC) activity in the skin of hairless mice, with an IC80 of 5.4 nmol per mouse[1].
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).
Molecular Weight

368.54

Formula

C23H28O2S
CAS No.
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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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AGN-191659 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AGN-191659156691-86-0AGN191659AGN 191659RAR/RXRRetinoic acid receptorsRetinoid X receptorsRAR/RXR agonistpromyelocytic leukemiahypertriglyceridemiaCDF (F-344)/CrlBR ratInhibitorinhibitorinhibit

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