For research use only. Not for therapeutic Use.
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].
SX-011 inhibits LPS stimulated TNFα and interleukin-1β (IL-1β) from human peripheral blood mononuclear cells (PBMC) with an IC50 of 200 nM and 900 nM, respectively. Additionally, IL-6 (IC50 250 nM) and IL-8 (IC50 100 nM) are significantly inhibited in this assay[2].
SX-011 is orally bioavailable in preclinical species (rat, 24%; monkey, 29%; dog, 43%) and has demonstrated efficacy in both acute and chronic models of inflammation in rats. Rat t1/2 = 30 min[1][2].
| Catalog Number | I010798 |
| CAS Number | 309913-42-6 |
| Synonyms | 2-[6-chloro-5-[4-[(4-fluorophenyl)methyl]piperidine-1-carbonyl]-1-methylindol-3-yl]-N,N-dimethyl-2-oxoacetamide |
| Molecular Formula | C26H27ClFN3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C26H27ClFN3O3/c1-29(2)26(34)24(32)21-15-30(3)23-14-22(27)20(13-19(21)23)25(33)31-10-8-17(9-11-31)12-16-4-6-18(28)7-5-16/h4-7,13-15,17H,8-12H2,1-3H3 |
| InChIKey | GUTYHDCSDBBMGW-UHFFFAOYSA-N |
| SMILES | CN1C=C(C2=CC(=C(C=C21)Cl)C(=O)N3CCC(CC3)CC4=CC=C(C=C4)F)C(=O)C(=O)N(C)C |
| 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. |
