CD 1530RAR receptor agonist CAS# 107430-66-0 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 107430-66-0 | SDF | Download SDF |
| PubChem ID | 9952709 | Appearance | Powder |
| Formula | C27H26O3 | M.Wt | 398.49 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 50 mM in 1eq. NaOH | ||
| Chemical Name | 4-[7-(1-adamantyl)-6-hydroxynaphthalen-2-yl]benzoic acid | ||
| SMILES | C1C2CC3CC1CC(C2)(C3)C4=C(C=C5C=CC(=CC5=C4)C6=CC=C(C=C6)C(=O)O)O | ||
| Standard InChIKey | VCQGNUWOMLYNNG-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C27H26O3/c28-25-12-22-6-5-21(19-1-3-20(4-2-19)26(29)30)10-23(22)11-24(25)27-13-16-7-17(14-27)9-18(8-16)15-27/h1-6,10-12,16-18,28H,7-9,13-15H2,(H,29,30) | ||
| 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 | Potent and selective RARγ receptor agonist (Ki values are 150, 1500 and 2750 nM for RARγ, RARβ and RARα receptors respectively). Activates transcriptional activity (AC50 = 1.8 nM). |
CD 1530 Dilution Calculator
CD 1530 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.5095 mL | 12.5474 mL | 25.0947 mL | 50.1895 mL | 62.7368 mL |
| 5 mM | 0.5019 mL | 2.5095 mL | 5.0189 mL | 10.0379 mL | 12.5474 mL |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5095 mL | 5.0189 mL | 6.2737 mL |
| 50 mM | 0.0502 mL | 0.2509 mL | 0.5019 mL | 1.0038 mL | 1.2547 mL |
| 100 mM | 0.0251 mL | 0.1255 mL | 0.2509 mL | 0.5019 mL | 0.6274 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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Target: RARγ, RARβ and RARα
Ki: 150, 1500, and 2750 nM
CD1530 is a potent and selective RAR receptor agonist with Ki values of 150, 1500 and 2750 nM for RARγ, RARβ and RARα receptors, respectively [1]. In addition, CD1530 shows moderate RARγ selectivity in the transcriptional assay with AC50 value of 1.8 nM. RAR-α is present in the majority of tissues while the distribution of RAR-β and γ is more selective [1]. RARγ mediated retinoic acid (RA)-induced growth arrest and apoptosis of neoplastic mouse papilloma cell lines [2].
In vitro: CD1530 inhibited excessive ROS production in tongue epithelial cells [2]. In addition, CD1530 was also a potent CYP26A1 inhibitor as ketoconazole with an IC50 value of 530 nM [3].
In vivo: The combination of the drugs bexarotene (300 mg/kg) and CD1530 (2.5 mg/100 mL in drinking water) was more effective than either drug alone in preventing oral carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide (4-NQO) in a mouse model of oral-cavity squamous-cell carcinoma (OCSCC), which did not cause cardiovascular risks [2]. High fat diet (HFD)-fed mice treated with CD1530 (2.5 mg/100 ml in drinking water) showed no decreases in steatosis, Kupffer cell TGF-β1 expression, or Hepatic stellate cells (HSCs) activation [4].
References:
1. Thacher SM, Vasudevan J, Chandraratna RA. Therapeutic applications for ligands of retinoid receptors. Curr Pharm Des. 2000;6(1):25-58.
2. Tang XH, Osei-Sarfo K, Urvalek AM, Zhang T, Scognamiglio T, Gudas LJ. Combination of bexarotene and the retinoid CD1530 reduces murine oral-cavity carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide. Proc Natl Acad Sci U S A. 2014;111(24):8907-12.
3. Thatcher JE, Buttrick B, Shaffer SA, Shimshoni JA, Goodlett DR, Nelson WL, et al. Substrate specificity and ligand interactions of CYP26A1, the human liver retinoic acid hydroxylase. Mol Pharmacol. 2011;80(2):228-39.
4. Trasino SE, Tang XH, Jessurun J, Gudas LJ. A retinoic acid receptor beta2 agonist reduces hepatic stellate cell activation in nonalcoholic fatty liver disease. J Mol Med (Berl). 2016.
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