Razuprotafib sodium  (Synonyms: AKB-9778 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)^[1].

Razuprotafib (AKB-9778) sodium promotes TIE2 phosphorylation and activation of downstream signaling in HUVECs and enhances angiopoietin-induced TIE2 phosphorylation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Razuprotafib sodium (20 mg/kg; s.c.) promotes phosphorylation of TIE2 in retinal endothelial cells in vivo^[1]. Razuprotafib sodium (10-20 mg/kg; s.c.; twice daily for 7 days) suppresses subretinal neovascularization (NV)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

608.68

C₂₆H₂₅N₄NaO₆S₃

1809275-69-1

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

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• [1]. Shen J, et al. Targeting VE-PTP activates TIE2 and stabilizes the ocular vasculature. J Clin Invest. 2014;124(10):4564-4576.  [Content Brief]