AC 55649 |
| Katalog-Nr.GC10871 |
AC 55649 ist ein potenter, hoch Isoform-selektiver Agonist des humanen RARβ2-Rezeptors mit einem pEC50 von 6,9.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 59662-49-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
AC 55649 is a potent and selective agonist of retinoic acid receptor β2 (RARβ2) isotype with a pEC50 value of 6.9 ± 0.4 [1].
RARβ2 is a tumor suppressor gene. In several human neoplasms, it is frequently hypermethylated [2].
In MCF7 cells, AC 55649 significantly inhibited cellular growth, appeared to inhibit DNA synthesis as seen in experiments of [3H] thymidine incorporation. The extent of the inhibition was comparable to the one resulted from the presence of all-trans-retinoic acid [1]. In vitro, RARβ2 induced the neurite outgrowth in adult mouse spinal cord [3]. Before neurite outgrowth, cells were stimulated with either AC 55649 or retinoic acid for 1 week. Treatment with retinoic acid largely increased the neurite outgrowth of cells, compared with the control. This result was revealed by immunocytochemistry. AC 55649 also induced the neurite outgrowth of NTERA-2 cells. This indicated that AC 55649 mediated neuronal differentiation in a manner similar to that found with retinoic acid. Using another differentiation marker, Neurofilament L, similar results were also evident [1].
Retinoids influence both differentiation and morphogenetic events during development of the vertebrate limb. These effects are mediated by nuclear retinoid receptors. In the posterior limb bud, transcripts of RARβ2 but not RARβ1 are enriched to three-fold. Transcripts of RARβ1 are initially present throughout the limb bud ectoderm and mesenchyme, then become restricted within the loose connective tissue and perichondrial regions of the limb [4]. In Xenopus, treated with AC 55649 at 100 nM, approximately 65% of larvae survived and practically all started to form a pair of bilaterally symmetric limb buds. Treatments with AC 55649 provoked the death of larvae at the metamorphosis onset at around stage 62. Stage 62 is a stage showing peak levels of T3 and T4 thyroid hormones. Meanwhile all larvae without treatment were metamorphosed [5].
References:
[1]. Piu F, Gauthier NK, Olsson R, et al. Identification of novel subtype selective RAR agonists. Biochemical pharmacology, 2005, 71(1): 156-162.
[2]. Jerónimo C, Henrique R, Hoque MO, et al. Quantitative RARβ2 Hypermethylation A Promising Prostate Cancer Marker. Clinical Cancer Research, 2004, 10(12): 4010-4014.
[3]. Maden M, Hind M. Retinoic acid, a regeneration-inducing molecule. Developmental dynamics, 2003, 226(2): 237-244.
[4]. Cuervo R, Chimal-Monroy J. Chemical activation of RARβ induces post-embryonically bilateral limb duplication during Xenopus limb regeneration. Scientific reports, 2013, 3.
[5]. Smith SM, Kirstein IJ, Wang ZS, et al. Differential expression of retinoic acid receptor-β isoforms during chick limb ontogeny. Developmental Dynamics, 1995, 202(1): 54-66.
| Cas No. | 59662-49-6 | SDF | |
| Chemical Name | 4'-octyl-[1,1'-biphenyl]-4-carboxylic acid | ||
| Canonical SMILES | OC(C1=CC=C(C=C1)C2=CC=C(C=C2)CCCCCCCC)=O | ||
| Formula | C21H26O2 | M.Wt | 310.44 |
| Löslichkeit | <31.04mg/ml in DMSO; <7.76mg/ml in ethanol | Storage | Store at -20°C |
| 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 | 3.2212 mL | 16.1062 mL | 32.2123 mL |
| 5 mM | 0.6442 mL | 3.2212 mL | 6.4425 mL |
| 10 mM | 0.3221 mL | 1.6106 mL | 3.2212 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *