| Bioactivity | SX 011 is a p38 inhibitor with IC50s of 9 nM and 90 nM against p38α and p38β, respectively. SX 011 also inhibits JNK-2 with an IC50 of 100 nM. SX-011 is orally bioavailable[1]. |
| Invitro | SX-011 抑制 LPS 刺激的人外周血单个核细胞 (PBMC) TNFα 和白细胞介素-1β (IL-1β)，IC50 分别为 200 nM 和 900 nM。此外，IL-6 (IC50 250 nM) 和 IL-8 (IC50 100 nM) 在该实验中被显著抑制[2]。 |
| In Vivo | SX-011 在临床前物种中具有口服利用率 (rat, 24%; monkey, 29%; dog, 43%)，并已证明对大鼠急性和慢性炎症模型均有效。Rat t1/2 = 30 min[1][2]。 |
| Name | SX 011 |
| CAS | 309913-42-6 |
| Formula | C26H27ClFN3O3 |
| Molar Mass | 483.96 |
| 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]. Lee MR, et al. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alpha protein. Curr Med Chem. 2005;12(25):2979-94. [2]. Hynes J Jr, et al. Small molecule p38 inhibitors: novel structural features and advances from 2002-2005. Curr Top Med Chem. 2005;5(10):967-85. |