BMS 961Selective RARγ agonist CAS# 185629-22-5 |
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Quality Control & MSDS
3D structure
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| Cas No. | 185629-22-5 | SDF | Download SDF |
| PubChem ID | 2418 | Appearance | Powder |
| Formula | C23H26FNO4 | M.Wt | 399.46 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO | ||
| Chemical Name | 3-fluoro-4-[[2-hydroxy-2-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)acetyl]amino]benzoic acid | ||
| SMILES | CC1(CCC(C2=C1C=CC(=C2)C(C(=O)NC3=C(C=C(C=C3)C(=O)O)F)O)(C)C)C | ||
| Standard InChIKey | AANFHDFOMFRLLR-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C23H26FNO4/c1-22(2)9-10-23(3,4)16-11-13(5-7-15(16)22)19(26)20(27)25-18-8-6-14(21(28)29)12-17(18)24/h5-8,11-12,19,26H,9-10H2,1-4H3,(H,25,27)(H,28,29) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective RARγ agonist (EC50 values are 30 and 1000 nM at RARγ and RARβ respectively). Displays no activity at RARα receptors. |
BMS 961 Dilution Calculator
BMS 961 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.5034 mL | 12.5169 mL | 25.0338 mL | 50.0676 mL | 62.5845 mL |
| 5 mM | 0.5007 mL | 2.5034 mL | 5.0068 mL | 10.0135 mL | 12.5169 mL |
| 10 mM | 0.2503 mL | 1.2517 mL | 2.5034 mL | 5.0068 mL | 6.2584 mL |
| 50 mM | 0.0501 mL | 0.2503 mL | 0.5007 mL | 1.0014 mL | 1.2517 mL |
| 100 mM | 0.025 mL | 0.1252 mL | 0.2503 mL | 0.5007 mL | 0.6258 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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BMS961 is a potent and selective retinoic acid receptor gamma (RARγ) agonist with IC50 values of 30 nM.
RARγ belongs to the family of nuclear receptors which regulates transcription. RARγ mediates the anti-proliferative and apoptotic effects of retinoids in cancer cells such as neuroblastoma cells. RARγ is the principal receptor that regulates RA mediated growth arrest in keratinocytes.
In vitro, application of BMS961on mouse ear skin was found to cause a significant increase of thymic stromal lymphopoietin (TSLP) transcripts1. In addition, exposure of BMS861 on limbs at low concentration leads to retarded growth of the zeugopod (long bones) and intactness of autopod (paw). However, high concentration of BMS961treatment caused equal undifferentiation of both limb regions 2.
In WT mice, RARγ agonists BMS961treatment resulted in an increase of the ear TSLP transcripts and serum TSLP, which indicates an involvement of RAR-mediated events in transcriptional activation of TSLP expression1.
References:
1. Li M, Hener P, Zhang Z, et al. Topical vitamin D3 and low-calcemic analogs induce thymic stromal lymphopoietin in mouse keratinocytes and trigger an atopic dermatitis. Proceedings of the National Academy of Sciences of the United States of America. 2006;103(31):11736-11741.
2. Galdones E, Hales BF. Retinoic acid receptor gamma-induced misregulation of chondrogenesis in the murine limb bud in vitro. Toxicological sciences : an official journal of the Society of Toxicology. 2008;106(1):223-232.
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Mouse P450RAI (CYP26) expression and retinoic acid-inducible retinoic acid metabolism in F9 cells are regulated by retinoic acid receptor gamma and retinoid X receptor alpha.[Pubmed:9442090]
J Biol Chem. 1998 Jan 23;273(4):2409-15.
We have cloned a mouse cDNA homolog of P450RAI, a cytochrome P450 belonging to a new family (CYP26), which has previously been isolated from zebrafish and human cDNAs and found to encode a retinoic acid-inducible retinoic acid hydroxylase activity. The cross-species conservation of the amino acid sequence is high, particularly between the mouse and the human enzymes, in which it is over 90%. Like its human and zibrafish counterparts, the mouse P450RAI cDNA catalyzes metabolism of retinoic acid into 4-OH-retinoic acid, 4-oxo-retinoic acid, 18-OH-retinoic acid, and unidentified water-soluble metabolites when transfected into COS-1 cells. Retinoic acid-inducible retinoic acid metabolism has previously been observed in F9 murine embryonal carcinoma cells and some derivatives lacking retinoid receptors. We were interested in determining whether P450RAI could be responsible for retinoic acid metabolism in F9 cells and in studying the effect of retinoid receptor ablation on P450RAI expression. In wild-type F9 cells and derivatives lacking RAR gamma, RAR alpha, and/or RXR alpha, we observed a direct relationship between the level of retinoic acid metabolic activity and retinoic acid-induced P450RAI mRNA. These experiments, as well as others using synthetic receptor subtype-specific retinoids, suggest that the RAR gamma and RXR alpha receptors mediate the effects of retinoic acid on the expression of the P450RAI gene.
