Razuprotafib
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) [1].
Product Specifications
CAS Number
[1008510-37-9]
Product Name Alternative
AKB-9778
UNSPSC
12352005
Target
Phosphatase; Tie
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease; Protein Tyrosine Kinase/RTK
Applications
COVID-19-immunoregulation
Field of Research
Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/razuprotafib.html
Concentration
10mM
Purity
99.18
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C([C@@H](NC(OC)=O)CC1=CC=CC=C1)N[C@H](C2=CSC(C3=CC=CS3)=N2)CC4=CC=C(NS(=O)(O)=O)C=C4
Molecular Formula
C26H26N4O6S3
Molecular Weight
586.70
References & Citations
[1]Shen J, et al. Targeting VE-PTP activates TIE2 and stabilizes the ocular vasculature. J Clin Invest. 2014;124 (10) :4564-4576.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Available Sizes
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