| Bioactivity | AL-438 is a potent, selective and orally active glucocorticoid receptor modulator with Kis of 2.5, 1786, 53, 1440, >1000 nM for glucocorticoid receptor, progesterone receptor, mineralocorticoid receptor, androgen receptor, estrogen receptor, respectively. AL-438 shows antiinflammatory activity[1][2]. |
| Target | Ki: 2.5 nM (glucocorticoid receptor) |
| Invitro | AL-438 (1 µM) 降低 ATDC5 细胞中 LPS 诱导的 IL-6 的生成[1]。AL-438 (0-1 µM; 1 h+24 h) 抑制 HSKF1501 细胞中 IL-1β (2 ng/ml) 诱导的 IL-6 表达[2]。 |
| In Vivo | AL-438 (1, 10, 100 mg/kg; p.o.) 在大鼠体内显示出抗炎活性[2]。 Animal Model: |
| Name | AL-438 |
| CAS | 239066-73-0 |
| Formula | C23H25NO2 |
| Molar Mass | 347.45 |
| 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]. Owen HC, et al. The growth plate sparing effects of the selective glucocorticoid receptor modulator, AL-438. Mol Cell Endocrinol. 2007 Jan 29;264(1-2):164-70. [2]. Coghlan MJ, et al. A novel antiinflammatory maintains glucocorticoid efficacy with reduced side effects. Mol Endocrinol. 2003 May;17(5):860-9. |