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205678-26-8

205678-26-8 Structure

205678-26-8 Structure
IdentificationBack Directory
[Name]

1H-2-Benzazepine-4-acetic acid, 2,3,4,5-tetrahydro-3-oxo-8-[3-(2-pyridinylamino)propoxy]-2-(2,2,2-trifluoroethyl)-, (4S)-
[CAS]

205678-26-8
[Synonyms]

SB-267268
1H-2-Benzazepine-4-acetic acid, 2,3,4,5-tetrahydro-3-oxo-8-[3-(2-pyridinylamino)propoxy]-2-(2,2,2-trifluoroethyl)-, (4S)-
[Molecular Formula]

C22H24F3N3O4
[MDL Number]

MFCD30533685
[MOL File]

205678-26-8.mol
[Molecular Weight]

451.44
Chemical PropertiesBack Directory
[Boiling point ]

677.2±55.0 °C(Predicted)
[density ]

1.320±0.06 g/cm3(Predicted)
[form ]

Solid
[pka]

4.32±0.10(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

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].
[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%.
[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. DOI:10.1167/iovs.05-1314
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