| CD 1530RAR receptor agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
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| Cas No. | 107430-66-0 | SDF | Download SDF |
| Chemical Name | 4-(7-((1s,3R,5S,7s)-adamantan-1-yl)-6-hydroxynaphthalen-2-yl)benzoic acid | ||
| Canonical SMILES | OC1=CC2=CC=C(C3=CC=C(C(O)=O)C=C3)C=C2C=C1[C@]4(C[C@H]5C6)C[C@@H](C5)C[C@H]6C4 | ||
| Formula | C27H26O3 | M.Wt | 398.49 |
| Solubility | Soluble in NaOH | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| 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. | ||
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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