SB-273005

SB-273005 is an orally active non-peptide αvβ3 integrin antagonist with K_i values of 1.2 nM and 0.3 nM for αvβ3 and αvβ5, respectively. SB-273005 blocks the binding of integrins to the RGD sequence in the extracellular matrix. SB-273005 inhibits Rictor phosphorylation and reduces IL-10 secretion. SB-273005 inhibits inflammation, prevents bone loss, regulates vascular smooth muscle function, and reverses pregnancy-induced immune deviation. SB-273005 can be used in the study of rheumatoid arthritis, osteoporosis, and aneurysms. ^{[1][2][3][4][5]}. In Vitro:SB-273005 (0.1 nM-1 µM; 1 h) dose-dependently inhibits adhesion of mouse and monkey VSMCs to vitronectin-coated plates, with similar IC₅₀ values (2.9 nM for mouse, 6.9 nM for monkey)^[2].
SB-273005 (100 nM-100 µM) inhibits TGFβ-induced Rictor phosphorylation and VSMC migration in mouse aortic smooth muscle cells^[3].
In Vivo:SB-273005 (10-60 mg/kg; p.o.; twice daily; 10-20 days) inhibits paw edema and protects joint integrity in rats with adjuvant-induced arthritis (AIA), as shown by reduced bone resorption and cartilage damage in DEXA, MRI, and histology analyses^[1].
SB-273005 (300-1000 mg/kg; p.o.; daily; 3-14 days) causes acute aortic and renal artery smooth muscle cell necrosis, followed by medial hypertrophy and fibrosis in CD-1 mice^[2].
SB-273005 (3 mg/kg; p.o.; during days 3-5 of pregnancy) reduces splenic Th2 cell polarization and IL-10 secretion, reversing pregnancy-induced immune deviation in pregnant mice^[4].
SB-273005 (3-30 mg/kg; p.o.; once daily; 8 days) decreases urinary deoxypyridinoline (bone resorption marker) and preserves trabecular bone density in Thyroxine-induced osteopenic rats^[5].