[8-[2-(6-Methylamino-pyridin-2-yl)-ethoxy]-3-oxo-2-(2,2,2-trifluoro-ethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl]-acetic acid
SB273005
CAS: 205678-31-5
Molecular Formula: C22H24F3N3O4
[8-[2-(6-Methylamino-pyridin-2-yl)-ethoxy]-3-oxo-2-(2,2,2-trifluoro-ethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl]-acetic acid - Names and Identifiers
[8-[2-(6-Methylamino-pyridin-2-yl)-ethoxy]-3-oxo-2-(2,2,2-trifluoro-ethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl]-acetic acid - Physico-chemical Properties
| Molecular Formula | C22H24F3N3O4 |
| Molar Mass | 451.44 |
| Density | 1.321±0.06 g/cm3(Predicted) |
| Boling Point | 662.9±55.0 °C(Predicted) |
| pKa | 4.32±0.10(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | In vitro, SB273005 inhibit human osteoclast-mediated bone experience with IC50 of 11 nM. In blood containing MDA-MB-231 cells, a combination of SB273005 and lamifiban inhibitors. In vitro, SB273005 inhibits human osteoclast-mediated bone resorption with an IC50 of 11 nM. In blood containing MDA-MB-231 cells, SB273005 combined with lamifiban inhibited tumor cell adhesion to the vascular extracellular matrix (ECM). |
| In vivo study | 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 anatomy of vascular smooth muscle cell (VSMC) in Aota and renal arteries of mice. In pregnant mice, SB273005 reverses the reduction of Th1 cell-produced IL-2 levels and the increment of Th2 cell-derived IL-10 levels. in a rat model of bone resorption and osteoporosis, SB273005 (30 mg/kg, p.o.) inhibits the parathyroid hormone-stimulated blood calcium response and inhibits bone loss. In adjuvant arthritis rats, SB273005 (60 mg/kg, p.o.) significantly reduced adjuvant-induced arthritis symptoms. In rat aortic and renal arteries, SB273005 (1000 mg/kg/day, p.o.) causes acute transient necrosis of vascular smooth muscle cells (VSMCs). In pregnant mice, SB273005 reversed the decrease in the IL-2 l level produced by Th1 cells and the increase in the IL-10 level derived from Th2 cells. |
[8-[2-(6-Methylamino-pyridin-2-yl)-ethoxy]-3-oxo-2-(2,2,2-trifluoro-ethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl]-acetic acid - Reference Information
| Biological activity | SB273005 is an effective integrin inhibitor. The Ki for αvβ3 receptor and αvβ5 receptor is 1.2 nM and 0.3 nM respectively. SB273005 is an effective integrin inhibitor. its Ki for αvβ3 receptor and αvβ5 receptor is 1.2 nM and 0.3 nM respectively. |
| in vitro study | 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 tumour cell adhesion to vascular extracellular matrix (ECM). in vitro, SB273005 inhibit bone resorption mediated by human osteoclasts, IC50 is 11 nM. In blood containing MDA-MB-231 cells, SB273005 combines with lamifiban to inhibit tumor cell adhesion to vascular extracellular matrix (ECM). |
| in vivo study | 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. in the rat model of bone resorption and osteoporosis, SB273005 (30 mg/kg, p.o.) inhibits parathyroid hormone-stimulated calcium response and bone loss. In adjuvant arthritis rats, SB273005 (60 mg/kg, p.o.) significantly reduced adjuvant-induced arthritis symptoms. In rat aorta and renal arteries, SB273005 (1000 mg/kg/day, p.o.) caused acute temporary necrosis of vascular smooth muscle cells (VSMC). In pregnant mice, SB273005 reversed the decrease in the level of IL-2 l produced by Th1 cells and the increase in the level of Th2 cell-derived IL-10. |
| target | TargetValue αvβ5 receptor (Cell-free assay) 0.3 nM αvβ3 receptor (Cell-free assay) 1.2 nM |
| Target | Value |
| αvβ5 receptor (Cell-free assay) | 0.3 nM |
| αvβ3 receptor (Cell-free assay) | 1.2 nM |
Last Update：2024-04-09 21:54:55
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Product Name: SB273005 Visit Supplier Webpage Request for quotation
CAS: 205678-31-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 205678-31-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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