| Description |
SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression[1].
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| Related Catalog |
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| In Vitro |
SB-267268 was much less potent for inhibition of human, mouse, and ratαvβ6 integrin. SB-267268 inhibits the attachment of bothαvβ3-transfected HEK293 cells to microtiter plate wells precoated with arginine-glycine-aspartic acid (RGD)-containing matrix proteins with IC50 values of 12 nM. SB-267268 also inhibits vitronectin-mediated human and rat aortic smooth-muscle-cell (SMC) migration with IC50 values of approximately 12.3 nM and 3.6 nM, respectively[1].
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| In Vivo |
SB-267268 (60 mg/kg; bi-daily, i.p.) reduces blood vessel profiles (BVPs) in the inner retina by 50%[1]. In ROP mice treated with SB-267268, VEGF and VEGFR-2 gene expression in the inner nuclear layer (INL) and the ganglion cell layer (GCL) is reduced[1]. Animal Model: Pregnant female C57BL/6 mice (ROP mice)[1] Dosage: 60 mg/kg Administration: I.p.; bi-daily Result: Reduced blood vessel profiles (BVPs) in the inner retina by 50%.
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| References |
[1]. Wilkinson-Berka JL, et al. SB-267268, a nonpeptidic antagonist of alpha(v)beta3 and alpha(v)beta5 integrins, reduces angiogenesis and VEGF expression in a mouse model of retinopathy of prematurity. Invest Ophthalmol Vis Sci. 2006 Apr;47(4):1600-5.
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