Razuprotafib sodium (AKB-9778) | VE-PTP inhibitor

Chemical Structure : Razuprotafib sodium

CAS No.: 1809275-69-1

Razuprotafib sodium (AKB-9778 sodium, AKB9778 sodium)

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

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

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2 mg	$218	In stock
5 mg	$358	In stock
10 mg	$548	In stock
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Biological Activity

Razuprotafib sodium (AKB-9778) 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.

Razuprotafib sodium (AKB-9778 sodium, AKB9778 sodium)

Biological Activity

Physicochemical Properties

References

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