BMS 493 (Synonyms: BMS 204493) |
Catalog No.GC15648
One-Click Copy Product Info
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Pan-RAR inverse agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 215030-90-3
Sample solution is provided at 25 µL, 10mM.
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BMS493 is an inverse agonist of pan-retinoic acid receptors (pan-RARs). This compound has been shown to increase nuclear corepressor (NCoR) interaction with RARs.
The retinoic acid receptor (RAR), a type of nuclear receptor , is a ligand-dependent transcription factor that is activated by 9-cis retinoic acid and all-trans retinoic acid. Binding of agonist ligands to RAR results in dissociation of corepressor and recruitment of coactivator protein that, in turn, promotes transcription of the downstream target gene into mRNA and eventually protein. This protein controls a number of physiological processes including cell growth, differentiation, survival, and death.
In cellular culture, pretreatment of BMS493 on MEPM cells blocked atRA-induced apoptotic indexes. Mechanistically, this component completely inhibited atRA-induced Sub-G1 fraction, DNA fragmentation, and caspase-3 activation.1.
In vivo, inhibition of RAR signaling with BMS493 induced a very high degree of congenital diaphragmatic hernia, which was associated with a marked left–right sidedness that depended on the timing of drug delivery2.
References:
1. Yu Z, Han J, Lin J, et al. Apoptosis induced by atRA in MEPM cells is mediated through activation of caspase and RAR. Toxicological sciences : an official journal of the Society of Toxicology. 2006;89(2):504-509.
2. Clugston RD, Zhang W, Alvarez S, et al. Understanding abnormal retinoid signaling as a causative mechanism in congenital diaphragmatic hernia. American journal of respiratory cell and molecular biology. 2010;42(3):276-285.
| Cas No. | 215030-90-3 | SDF | |
| Synonyms | BMS 204493 | ||
| Chemical Name | (E)-4-(2-(5,5-dimethyl-8-(phenylethynyl)-5,6-dihydronaphthalen-2-yl)vinyl)benzoic acid | ||
| Canonical SMILES | OC(C1=CC=C(C=C1)/C=C/C2=CC=C3C(C)(C)CC=C(C#CC4=CC=CC=C4)C3=C2)=O | ||
| Formula | C29H24O2 | M.Wt | 404.5 |
| Solubility | 25mg/mL in DMSO, 30mg/mL in DMF | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4722 mL | 12.3609 mL | 24.7219 mL |
| 5 mM | 494.4 μL | 2.4722 mL | 4.9444 mL |
| 10 mM | 247.2 μL | 1.2361 mL | 2.4722 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 saline, 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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)