1809275-69-1
Chemical Structure
Razuprotafib sodium
Synonym(s): AKB-9778 sodium
- CAS No.: 1809275-69-1
- Formula:C26H25N4NaO6S3
- Molecular Weight:608.68
IUPAC Name: (4-((S)-2-((S)-2-((methoxycarbonyl)amino)-3-phenylpropanamido)-2-(2-(thiophen-2-yl)thiazol-4-yl)ethyl)phenyl)sulfamic acid, sodium salt
InChIKey: FXNDNMZPAYMZNC-GUTACTQSSA-M
SMILES: O=S(NC(C=C1)=CC=C1C[C@@H](C2=CSC(C3=CC=CS3)=N2)NC([C@@H](NC(OC)=O)CC4=CC=CC=C4)=O)(O[Na])=O
Biological Activity: Razuprotafib (AKB-9778) sodium is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib sodium promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib sodium inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib sodium shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM)[1].
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Razuprotafib sodium | Razuprotafib (AKB-9778) sodium is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib sodium promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib sodium inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib sodium shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM). | |||||||||||||||||||||
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Keywords
