Information SB273005 SB273005 is a potent integrin inhibitor with K i of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively. Targets αvβ5 receptor (Cell-free assay); αvβ3 receptor (Cell-free assay) 0.3 nM; 1.2 nM In vitro SB273005 inhibits human osteoclast-mediated bone resorption with IC50 of 11 nM. In blood containing MDA-MB-231 cells, a combination of SB273005 and lamifiban inhibits tumor cell adhesion to vascular extracellular matrix (ECM). In vivo In rat models of bone resorption and osteoporosis, SB273005 (30 mg/kg, p.o.) inhibits the parathyroid hormone-stimulated calcemic response, and inhibits bone loss. In rat with adjuvant-induced arthritis, SB273005 (60 mg/kg, p.o.) significantly reduces the symptoms of adjuvant-induced arthritis. SB273005 (1000 mg/kg/day, p.o.) causes acute, transient necrosis of vascular smooth muscle cell (VSMC) in aorta and renal arteries of mice. In pregnant mice, SB273005 reverses the reduction of Th1 cell-produced IL-2 levels and the increase of Th2 cell-derived IL-10 levels.
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SB273005
CAS number:205678-31-5 molecular formula:C22H24F3N3O4
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| Chinese alias | - | ||
| English alias | (S)-2-(8-(2-(6-(Methylamino)pyridin-2-yl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl)acetic acid | (S)-8-[2-[6-(methylamino)pyridin-2-yl]-1-ethoxy]-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-a | ||
| CAS number | 205678-31-5 | molecular formula | C22H24F3N3O4 |
| molecular weight | 451.44 g/mol | Exact mass | ≥99% |
| PSA | 91.800 Ų | logp | 3.364 |
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