| Bioactivity | RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA2 of 8.06. RXR antagonist 1 can be used for type 2 diabetes research[1]. |
| Invitro | RXR antagonist 1 (compound 6a) shows potent RXR-antagonistic activities at 1 μM[1].RXR antagonist 1 shows competitive binding to the LBP in hRXRα-LBD, with Ki of 0.384 ± 0.072, Kd of 0.277 ± 0.038, and Ki/Kd of 1.39[1].The cell permeability of RXR antagonist 1 shows no correlation with RXR-antagonistic activity[1]. |
| Name | RXR antagonist 1 |
| Formula | C28H33F3N2O3 |
| Molar Mass | 502.57 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Masaki Watanabe, et al. Increased Molecular Flexibility Widens the Gap between Ki and Kd values in Screening for Retinoid X Receptor Modulators. ACS Med. Chem. Lett. 2022, 13, 2, 211-217. |