AC 261066 |
Catalog No.GC11852 |
Potent RARβ2 agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 870773-76-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
AC 261066 is an agonist of retinoic acid receptor subtype β isoform 2 (RARβ2) [1] [2]. It is also called UVI2062 [3]. AC 261066 exhibited good oral bioavailability in rats (Foral= 52%) [4]. The IC50 of AC 261066 to AKR1B10 is 51 ± 7µM. No inhibition of AC 261066 to AKR1B1 was detected when using up to 100 µM AC 261066 in the enzymatic assay [3].
Retinoic acid receptors (RARs, subtypes α, β, γ) form heterodimeric complexes with retinoid X receptors (RXR α, β, γ) to orchestrate complex events, such as organ homoeostasis, immune function, development and reproduction [1]. RARβ2 is an isoform of subtype β of retinoic acid receptor, its affinity to retinoids and biological functions are different from other isoforms [2].
AC 261066 did not induce the cell adhesion of RPMI 8866 B cells to the ADAM28 disintegrin-like domain and did not block the atRA-induced adhesion [5].
AC 261066-treatment significantly inhibited the tail regeneration process in N. viridescens compared to DMSO controls. When these AC 261066-treated newts were removed from AC 261066 at 21 days (time of analysis) and then placed back into normal pond water, tail regeneration commenced. Five weeks after removal from the AC 26l066, the tail had regenerated, albeit with an alteration in the dorsal-ventral patterning compared to a normal tail regenerate [6].
References:
[1]. Albane le Maire, Susana Álvarez, Pattabhiraman Shankaranarayanan, et al. Retinoid Receptors and Therapeutic Applications of RAR/RXR Modulators. Current Topics in Medicinal Chemistry, 2012, 12: 505-527.
[2]. Christopher R. Gardner, Belamy B. Cheung, Jessica Koach, et al. Synthesis of retinoid enhancers based on 2-aminobenzothiazoles for anti-cancer therapy. Bioorg. Med. Chem., 2012, 20: 6877-6884.
[3]. Sergio Porté, Joan Giménez, Marta Dominguez, et al. Aldo–keto reductases in retinoid metabolism: Search for substrate specificity and inhibitor selectivity. Chemico-Biological Interactions, 2013, 202(1-3):186-94.
[4]. Birgitte W. Lund, Fabrice Piu, Natalie K. Gauthier, et al. Discovery of a Potent, Orally Available, and Isoform-Selective Retinoic Acid β2 Receptor Agonist. J. Med. Chem., 2005, 48: 7517-7519.
[5]. Jarrett T. Whelan, Lei Wang, Jianming Chen, et al. Retinoids induce integrin-independent lymphocyte adhesion through RAR-α nuclear receptor activity. Biochemical and Biophysical Research Communications, 2014, 454: 537-542.
[6]. Christopher J. Carter. Identification of novel retinoid receptors and their roles in vertebrate and invertebrate nervous systems [D]. St. Catharines: Brock University, 2011.
Cas No. | 870773-76-5 | SDF | |
Chemical Name | 4-(4-(2-butoxyethoxy)-5-methylthiazol-2-yl)-2-fluorobenzoic acid | ||
Canonical SMILES | FC1=CC(C2=NC(OCCOCCCC)=C(C)S2)=CC=C1C(O)=O | ||
Formula | C17H20FNO4S | M.Wt | 353.41 |
Solubility | <35.34mg/ml in DMSO; <35.34mg/ml in ethanol | Storage | Store at RT |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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 | 0.283 mL | 1.4148 mL | 2.8296 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
(Based on Reviews and 36 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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