| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
AGN 192870 targets retinoic acid receptors (RARs), including RARα, RARβ, and RARγ, functioning as a neutral antagonist. It shows Kd values of 147 nM for RARα, 33 nM for RARβ, and 42 nM for RARγ. The compound shows IC₅₀ values of 87 nM for RARα and 32 nM for RARγ. It displays RARβ partial agonism. By modulating RAR activity, the compound influences cell growth, differentiation, and apoptosis. Its neutral antagonist profile makes it a valuable tool for studying RAR-mediated signaling pathways.
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| ln Vitro |
In vitro, AGN 192870 demonstrates potent RAR antagonist activity. It shows Kd values of 147 nM for RARα, 33 nM for RARβ, and 42 nM for RARγ. The compound shows IC₅₀ values of 87 nM for RARα and 32 nM for RARγ. It displays RARβ partial agonism. The compound's activity is assessed in cell-based reporter assays using RAR response element (RARE)-luciferase constructs. It can be used to study cell growth arrest, differentiation, and apoptosis. Its click chemistry capability allows for further functionalization and study.
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| ln Vivo |
Specific in vivo activity data for AGN 192870 are not extensively documented in the publicly available literature. As a potent RAR antagonist, the compound has potential applications in studying RAR-mediated biological processes including development, differentiation, and apoptosis. Its neutral antagonist profile may offer advantages over agonists or inverse agonists for certain research applications. The compound's click chemistry capability may enable in vivo labeling or targeting studies. Further in vivo studies are needed to fully characterize its efficacy and safety.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for AGN 192870 typically involve competitive binding experiments using RAR proteins (RARα, RARβ, RARγ) and radiolabeled or fluorescently labeled retinoic acid as tracer. The compound's binding affinity to each RAR subtype is assessed, with Kd values of 147 nM for RARα, 33 nM for RARβ, and 42 nM for RARγ. IC₅₀ values of 87 nM for RARα and 32 nM for RARγ are determined. Assays are conducted in buffered solutions at physiological pH with appropriate receptor preparations.
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| Cell Assay |
In vitro cell-based assays for AGN 192870 utilize cell lines expressing RARs to assess its antagonist activity. Cells are treated with varying concentrations of the compound for 24-48 hours. RAR-mediated transcriptional activity is evaluated using reporter gene assays with RARE-luciferase constructs. The compound's antagonist activity is assessed by its ability to inhibit retinoic acid-induced transcriptional activation. Its RARβ partial agonism is confirmed through dose-response experiments. Cell growth, differentiation, and apoptosis can be assessed using appropriate assays. Standard cell culture conditions (37°C, 5% CO₂) with appropriate media are employed.
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| Animal Protocol |
In vivo animal studies with AGN 192870 would typically involve administration of the compound to rodent models to evaluate its effects on RAR-mediated processes. Potential study designs include models of development, differentiation, or cancer where RAR signaling plays a role. Typical endpoints would include assessment of differentiation markers, cell proliferation, apoptosis, and pharmacokinetic profiling. The compound's click chemistry capability may enable in vivo labeling studies. All procedures must comply with institutional animal care and use guidelines.
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| ADME/Pharmacokinetics |
AGN 192870 has a molecular weight of 378.46 g/mol and a molecular formula of C₂₇H₂₂O₂. Its chemical name is 4-[2-(5,5-dimethyl-8-phenyl-6H-naphthalen-2-yl)ethynyl]benzoic acid. It is a potent RAR neutral antagonist with Kd values of 147 nM (RARα), 33 nM (RARβ), and 42 nM (RARγ). It shows IC₅₀ values of 87 nM (RARα) and 32 nM (RARγ). It contains an alkyne group for click chemistry applications. The compound is typically stored under conditions recommended for research chemicals.
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| Toxicity/Toxicokinetics |
AGN 192870 is intended for research use only and is not approved for human therapeutic applications. As a research chemical, comprehensive toxicological data are not available in the publicly accessible literature. Standard safety precautions should be observed when handling this compound, including the use of appropriate personal protective equipment. As with all research chemicals, comprehensive toxicological profiling would be required before any consideration for clinical development.
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| References | |
| Additional Infomation |
AGN 192870 (CAS#: 166977-57-7) has a molecular formula of C₂₇H₂₂O₂ and a molecular weight of 378.46 g/mol. Its chemical name is 4-[2-(5,5-dimethyl-8-phenyl-6H-naphthalen-2-yl)ethynyl]benzoic acid. It is a potent RAR neutral antagonist with Kd values of 147 nM (RARα), 33 nM (RARβ), and 42 nM (RARγ). It shows IC₅₀ values of 87 nM (RARα) and 32 nM (RARγ). It displays RARβ partial agonism. The compound contains an alkyne group for click chemistry. It is used to study cell growth arrest, differentiation, and apoptosis. This compound is not a drug and has not undergone clinical trials.
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| Molecular Formula |
C27H22O2
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|---|---|
| Molecular Weight |
378.46238
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| Exact Mass |
378.161
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| CAS # |
166977-57-7
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| PubChem CID |
10339622
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
6.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
689
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC(C1=CC=C(C#CC2C=CC3C(CC=C(C4=CC=CC=C4)C=3C=2)(C)C)C=C1)=O
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| InChi Key |
LTHJFFPLLKIZTC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H22O2/c1-27(2)17-16-23(21-6-4-3-5-7-21)24-18-20(12-15-25(24)27)9-8-19-10-13-22(14-11-19)26(28)29/h3-7,10-16,18H,17H2,1-2H3,(H,28,29)
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| Chemical Name |
4-[2-(5,5-dimethyl-8-phenyl-6H-naphthalen-2-yl)ethynyl]benzoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 6.25 mg/mL (16.51 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6423 mL | 13.2114 mL | 26.4229 mL | |
| 5 mM | 0.5285 mL | 2.6423 mL | 5.2846 mL | |
| 10 mM | 0.2642 mL | 1.3211 mL | 2.6423 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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