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Integrin Antagonist 1 (hydrochloride)

Names

[ CAS No. ]:
1629249-40-6

[ Name ]:
Integrin Antagonist 1 (hydrochloride)

[Synonym ]:
(3S)-3-[3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl]-4-{(3R)-3-[2-(1,5,6,7-tetrahydro-1,8-naphthyridin-2-yl)ethyl]-1-pyrrolidinyl}butanoic acid hydrochloride (1:1)
1-Pyrrolidinebutanoic acid, β-[3-(3,5-dimethyl-1H-pyrazol-1-yl)phenyl]-3-[2-(1,5,6,7-tetrahydro-1,8-naphthyridin-2-yl)ethyl]-, (βS,3R)-, hydrochloride (1:1)
Integrin Antagonist 1 (hydrochloride)

Biological Activity

[Description]:

GSK 3008348 (hydrochloride) is a small molecule integrin αvβ6 antagonist, extracted from patent WO/2014154725A1, example 1. The affinity (pIC50) for the human - a 6 protein in the Fluorescence Polarisation Assay for GSK 3008348 (hydrochloride) is 8.1, whereas its affinity in the cell Adhesion Assays was for: ανβ6 (pIC50 = 8.4); ανβ3 (pIC50 = 6); ανβ5 (pIC50 = 6.9); ανβ8 (pIC50 = 7.7).

[Related Catalog]:

Signaling Pathways >> Cytoskeleton >> Integrin
Research Areas >> Cardiovascular Disease

[Target]

pIC50 value: 8.4 (αvβ6)[1].


[References]

[1]. Anderson Niall Andrew, et al. Preparation of naphthyridine derivatives useful as αvβ6 integrin antagonists. From PCT Int. Appl. (2014), WO 2014154725 A1 20141002.


[Related Small Molecules]

Cilengitide | Cyclo(-Arg-Gly-Asp-D-Phe-Lys) trifluoroacetate salt | Arg-Gly-Asp-Ser | CWHM-12 | OSU-T315 | E 7820 | GLPG 0187 | Firategrast | ATN-161 trifluoroacetate salt | Cucurbitacin B | Eptifibatide acetate salt | iRGD peptide | Lifitegrast | Zaurategrast | TR 14035

Chemical & Physical Properties

[ Molecular Formula ]:
C29H37N5O2.xHCl

[ Molecular Weight ]:
524.097

[ Exact Mass ]:
523.271423

Related Compounds

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