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Razuprotafib sodium

Chemical Structure : Razuprotafib sodium

CAS No.: 1809275-69-1

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Razuprotafib sodium (AKB-9778 sodium, AKB9778 sodium)

Catalog No.: PC-60081Not For Human Use, Lab Use Only.

AKB-9778 (Razuprotafib) sodium is a potent, selective inhibitor of vascular endothelial protein tyrosine phosphatase (VE-PTP, HPTPβ) with IC50 of 17 pM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AKB-9778 (Razuprotafib) sodium is a potent, selective inhibitor of vascular endothelial protein tyrosine phosphatase (VE-PTP, HPTPβ) with IC50 of 17 pM.
AKB-9778 shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (IC50=100 pM).
AKB-9778 activates TIE2, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK.
AKB-9778 blocks VEGF-induced leakage from dermal and retinal vessels and prevents exudative retinal detachments in double-transgenic mice.

Physicochemical Properties

M.Wt 608.68
Formula C26H25N4NaO6S3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(4-{(2S)-2-{(2S)-2-[(methoxycarbonyl)amino]-3-phenylpropanamido}-2-[2-(thiophen-2-yl)-1,3-thiazol-4-yl]ethyl}phenyl)sulfamic acid, sodium salt

References

1. Goel S, et al. J Natl Cancer Inst. 2013 Aug 21;105(16):1188-201.
2. Shen J, et al. J Clin Invest. 2014 Oct;124(10):4564-76.
3. Amarasinghe KK, et al. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4252-6.

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