化学性质：                                                                                                             

产品描述：                                                                                                            

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].

特别提醒：