AGN 205728RARγ antagonist,potent and selective CAS# 859498-05-8 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 859498-05-8 | SDF | Download SDF |
| PubChem ID | 11419220 | Appearance | Powder |
| Formula | C29H27NO3 | M.Wt | 437.53 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc. | ||
| Chemical Name | 4-[(E,3E)-3-[8,8-dimethyl-5-(4-methylphenyl)-7H-naphthalen-2-yl]-3-hydroxyiminoprop-1-enyl]benzoic acid | ||
| SMILES | CC1=CC=C(C=C1)C2=CCC(C3=C2C=CC(=C3)C(=NO)C=CC4=CC=C(C=C4)C(=O)O)(C)C | ||
| Standard InChIKey | AUKGBKLQWDXBEP-FSLFYVJCSA-N | ||
| Standard InChI | InChI=1S/C29H27NO3/c1-19-4-9-21(10-5-19)24-16-17-29(2,3)26-18-23(13-14-25(24)26)27(30-33)15-8-20-6-11-22(12-7-20)28(31)32/h4-16,18,33H,17H2,1-3H3,(H,31,32)/b15-8+,30-27+ | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/ 0.6 nM; no inhibiton on RARα and RARβ.
IC50 value: 3 nM/ 0.6 nM(Ki/IC95)
Target: RARγ antagonist
More information can be found in the following patent, Compound 7a.
Preparation of disubstituted chalcone oximes having RARγ retinoid receptor antagonist activity
By Tsang, Kwok Yin; Sinha, Santosh; Liu, Xiaoxia; Bhat, Smita; Chandraratna, Roshantha A.
From PCT Int. Appl. (2005), WO 2005066115 A2 20050721. References: | |||||
AGN 205728 Dilution Calculator
AGN 205728 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2856 mL | 11.4278 mL | 22.8556 mL | 45.7112 mL | 57.1389 mL |
| 5 mM | 0.4571 mL | 2.2856 mL | 4.5711 mL | 9.1422 mL | 11.4278 mL |
| 10 mM | 0.2286 mL | 1.1428 mL | 2.2856 mL | 4.5711 mL | 5.7139 mL |
| 50 mM | 0.0457 mL | 0.2286 mL | 0.4571 mL | 0.9142 mL | 1.1428 mL |
| 100 mM | 0.0229 mL | 0.1143 mL | 0.2286 mL | 0.4571 mL | 0.5714 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/ 0.6 nM; no inhibiton on RARα and RARβ.
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Complexes of DNA bases and Watson-Crick base pairs interaction with neutral silver Agn (n = 8, 10, 12) clusters: a DFT and TDDFT study.[Pubmed:28325114]
J Biomol Struct Dyn. 2018 Mar;36(4):1050-1062.
We study the binding of the neutral Agn (n = 8, 10, 12) to the DNA base-adenine (A), guanine (G) and Watson-Crick -adenine-thymine, guanine-cytosine pairs. Geometries of complexes were optimized at the DFT level using the hybrid B3LYP functional. LANL2DZ effective core potential was used for silver and 6-31 + G(**) was used for all other atoms. NBO charges were analyzed using the Natural population analysis. The absorption properties of Agn-A,G/WC complexes were also studied using time-dependent density functional theory. The absorption spectra for these complexes show wavelength in the visible region. It was revealed that silver clusters interact more strongly with WC pairs than with isolated DNA complexes. Furthermore, it was found that the electronic charge transferred from silver to isolated DNA clusters are less than the electronic charge transferred from silver to the Agn-WC complexes. The vertical ionization potential, vertical electron affinity, hardness, and electrophilicity index of Agn-DNA/WC complexes have also been discussed.
Decursin in Angelica gigas Nakai (AGN) Enhances Doxorubicin Chemosensitivity in NCI/ADR-RES Ovarian Cancer Cells via Inhibition of P-glycoprotein Expression.[Pubmed:27605402]
Phytother Res. 2016 Dec;30(12):2020-2026.
Angelica gigas Nakai (AGN, Korean Dang-gui) is traditionally used for the treatment of various diseases including cancer. Here, we investigated multidrug-resistant phenotype-reversal activities of AGN and its compounds (decursin, ferulic acid, and nodakenin) in doxorubicin-resistant NCI/ADR-RES ovarian cancer cells. Our results showed that a combination of doxorubicin with either AGN or decursin inhibited a proliferation of NCI/ADR-RES cells. These combinations increased the number of cells at sub-G1 phase when cells were stained with Annexin V-fluorescein isothiocyanate. We also found that these combinations activated caspase-9, caspase-8, and caspase-3 and increased cleaved PARP level. Moreover, an inhibition of P-glycoprotein expression by either AGN or decursin resulted in a reduction of its activity in NCI/ADR-RES cells. Therefore, our data demonstrate that decursin in AGN inhibits doxorubicin-resistant ovarian cancer cell proliferation and induces apoptosis in the presence of doxorubicin via blocking P-glycoprotein expression. Therefore, AGN would be a potentially novel treatment option for multidrug-resistant tumors by sensitizing to anticancer agents. Copyright (c) 2016 John Wiley & Sons, Ltd.
Anti-cancer and other bioactivities of Korean Angelica gigas Nakai (AGN) and its major pyranocoumarin compounds.[Pubmed:22583405]
Anticancer Agents Med Chem. 2012 Dec;12(10):1239-54.
Korean Angelica gigas Nakai (AGN) is a major medicinal herb used in Asian countries such as Korea and China. Traditionally, its dried root has been used to treat anemia, pain, infection and articular rheumatism in Korea, most often through boiling in water to prepare the dosage forms. The pyranocoumarin compound decursin and its isomer decursinol angelate (DA) are the major chemical components in the alcoholic extracts of the root of AGN. The in vitro anti-tumor activities of decursin and/or DA against prostate cancer, lung cancer, breast cancer, colon cancer, bladder cancer, sarcoma, myeloma and leukemia have been increasingly reported in the past decade whereas the in vivo efficacy in mouse models was established only for a few organ sites. Preliminary pharmacokinetic studies by us and others in rodent models indicated that decursinol (DOH), which has much less in vitro direct anticancer activities by itself, is the major and rapid in vivo hydrolysis metabolite of both decursin and DA. Besides decursin, DA and DOH, other chemical components in AGN such as polysaccharides and polyacetylenes have been reported to exert anti-cancer and anti-inflammation activities as well. We systematically reviewed the published literature on the anti-cancer and other bio-activities effects of AGN extract and decursin, DA and DOH, as well as other chemicals identified from AGN. Although a number of areas are identified that merit further investigation, one critical need is first-in-human studies of the pharmacokinetics of decursin/DA to determine whether humans differ from rodents in absorption and metabolism of these compounds.
Usefulness of Chromogenic CromoCen(R) AGN agar medium for the identification of the genus Aeromonas: Assessment of faecal samples.[Pubmed:22561188]
J Microbiol Methods. 2012 Aug;90(2):100-4.
Selective screening media for the detection and identification of Aeromonas strains are needed to guide primary isolation procedures in the clinical laboratory. This study compared the selective CromoCen(R) AGN chromogenic agar medium for the detection and identification of Aeromonas strains that were isolated from various samples against the conventional selective agar media that are commonly used for the isolation of this organism in food, environmental and clinical samples. The Miles and Misra and ecometric methods were used to evaluate the microbiological performance of CromoCen(R) AGN chromogenic agar medium, which was shown to be satisfactory. A total of 14 reference Aeromonas strains, 44 wild strains and 106 clinical stool specimens were examined using both non-chromogenic selective agars that are commonly used for Aeromonas isolation and CromoCen(R) AGN agar. The latter exhibited 94.73% sensitivity and 100% specificity for the various samples. On CromoCen(R) AGN agar medium, Aeromonas formed colonies with light green, greenish and salmon pigments with or without a surrounding wide transparent zone (halo) of 2-3mm in diameter around the entire border. This medium is recommended for the isolation and potential identification of the Aeromonas genus.
