SB273005 是一种有效的整合素抑制剂，对 αvβ3 受体和 αvβ5 受体的 Ki 分别为 1.2 nM 和 0.3 nM。

SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.

In vitro, SB273005 inhibits human osteoclast-mediated bone resorption with IC50 of 11 nM. [1] In blood containing MDA-MB-231 cells, a combination of SB273005 and lamifiban inhibits tumor cell adhesion to vascular extracellular matrix (ECM). [3]

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. [1] In rat with adjuvant-induced arthritis, SB273005 (60 mg/kg, p.o.) significantly reduces the symptoms of adjuvant-induced arthritis. [2] SB273005 (1000 mg/kg/day, p.o.) causes acute, transient necrosis of vascular smooth muscle cell (VSMC) in aorta and renal arteries of mice. [4] In pregnant mice, SB273005 reverses the reduction of Th1 cell-produced IL-2 levels and the increase of Th2 cell-derived IL-10 levels. [5]

205678-31-5

C22H24F3N3O4

451.446

DMSO:83 mg/mL (183.9 mM)
H2O:<1 mgml
Ethanol:10 mg/mL(22.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years