| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
AC-261066 targets the retinoic acid receptor beta 2 (RARβ2), a nuclear receptor that regulates gene expression in response to retinoic acid. RARβ2 is involved in various physiological processes, including cell differentiation, proliferation, and apoptosis. AC-261066 is an isoform-selective agonist that specifically activates RARβ2 with high potency. Its selectivity for RARβ2 over RARβ1, RARα, and RARγ makes it a valuable tool for studying the specific functions of RARβ2.
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| ln Vitro |
In port (F oral = 52%), AC-261066 has good oral bioavailability [1].
In vitro, AC-261066 demonstrates potent agonist activity at RARβ2 with a pEC50 of 8.0-8.1. It exhibits selectivity over RARβ1 (pEC50 = 6.4), RARα (pEC50 = 6.2), and RARγ (pEC50 = 6.3). The compound's potency and selectivity have been confirmed in various in vitro assays, including reporter gene assays and binding studies. AC-261066 is more potent than AC 55649. |
| ln Vivo |
In vivo, AC-261066 exhibits good oral bioavailability in rats, with a reported Foral of 52%. The compound is orally available and has been shown to be effective in preclinical models. Its in vivo activity is consistent with its potent in vitro agonist activity at RARβ2. Detailed in vivo efficacy data from specific animal models are limited in publicly available sources but are supported by the compound's oral bioavailability and preclinical characterization.
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| Enzyme Assay |
In non-cell-based receptor binding assays, AC-261066's affinity for RARβ2 is evaluated using radioligand competition binding experiments. Nuclear receptor preparations or purified RAR proteins are incubated with a radiolabeled RAR ligand and varying concentrations of AC-261066. After incubation, bound and free radioligand are separated, and radioactivity is measured. Competition curves are generated to determine IC50 and Ki values, confirming the compound's potent binding affinity for RARβ2.
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| Cell Assay |
In vitro cellular assays for AC-261066 involve measuring its agonist activity at RARβ2 using reporter gene assays. Cells are transfected with a reporter construct containing a retinoic acid response element (RARE) upstream of a luciferase or other reporter gene, along with expression constructs for RARβ2 and its heterodimer partner RXR. Cells are treated with AC-261066, and reporter activity is measured to quantify RARβ2 activation. These assays have established AC-261066's pEC50 of 8.0-8.1 and its selectivity profile.
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| Animal Protocol |
In vivo animal studies for AC-261066 have been conducted in rat models to evaluate its oral bioavailability and pharmacological effects. The compound exhibited good oral bioavailability (Foral = 52%) in rats. Specific efficacy studies in animal models of diseases relevant to RARβ2 signaling would be required to fully characterize its therapeutic potential. The compound's oral availability makes it suitable for in vivo studies.
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| ADME/Pharmacokinetics |
AC-261066 has demonstrated good oral bioavailability in rats, with a Foral of 52%. The compound is soluble in DMSO at 35.34 mg/mL. Storage conditions for the powder are -20°C for 3 years or 4°C for 2 years; in solvent, it can be stored at -80°C for 6 months or -20°C for 1 month. The compound's pharmacokinetic profile supports its use in oral administration studies.
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| Toxicity/Toxicokinetics |
Toxicological data for AC-261066 are limited in publicly available sources. As a research compound intended for laboratory use, comprehensive toxicology studies have not been extensively published. The compound is not intended for human use and should be handled with appropriate safety precautions. Its safety profile is consistent with that of other research chemicals used in preclinical studies.
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| References | |
| Additional Infomation |
AC-261066 is a potent, orally available, and isoform-selective RARβ2 agonist with a pEC50 of 8.0-8.1. It is selective over RARβ1, RARα, and RARγ. The compound has demonstrated good oral bioavailability in rats (Foral = 52%). AC-261066 is more potent and orally available than AC 55649. It is a research chemical and is not an approved drug.
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| Molecular Formula |
C17H20NO4FS
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|---|---|
| Molecular Weight |
353.4084
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| Exact Mass |
353.11
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| CAS # |
870773-76-5
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| PubChem CID |
11530459
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.151
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
24
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| Complexity |
401
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HSAOETBFVAWNRP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20FNO4S/c1-3-4-7-22-8-9-23-15-11(2)24-16(19-15)12-5-6-13(17(20)21)14(18)10-12/h5-6,10H,3-4,7-9H2,1-2H3,(H,20,21)
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| Chemical Name |
4-[4-(2-butoxyethoxy)-5-methyl-1,3-thiazol-2-yl]-2-fluorobenzoic 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 : ~50 mg/mL (~141.48 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8296 mL | 14.1479 mL | 28.2957 mL | |
| 5 mM | 0.5659 mL | 2.8296 mL | 5.6591 mL | |
| 10 mM | 0.2830 mL | 1.4148 mL | 2.8296 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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