Razuprotafib free base

Razuprotafib is a potent and selective inhibitor of the catalytic activity of VE-PTP.

For research use only. Not for human or veterinary use.

Target Phosphatase Tie

Research area Inflammation/Immunology

Purity >98% Stock Inquire

Data Sheet SDS COA

Razuprotafib structure

CAS No.: 1008510-37-9

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 1,175.00	BP-00054-500mg	In stock	Get quote
1 g	USD 1,780.00	BP-00054-1g	In stock	Get quote

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Description

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).

Biological activity

In Vitro Razuprotafib (AKB-9778) promotes TIE2 phosphorylation and activation of downstream signaling in HUVECs and enhances angiopoietin-induced TIE2 phosphorylation. In Vivo Razuprotafib (20 mg/kg; s.c.) promotes phosphorylation of TIE2 in retinal endothelial cells in vivo[1]. Razuprotafib (10-20 mg/kg; s.c.; twice daily for 7 days) suppresses subretinal neovascularization (NV).

Identifiers

SMILES: [C@@H](CC1=CC=C(NS(=O)(=O)O)C=C1)(NC([C@H](CC2=CC=CC=C2)NC(OC)=O)=O)C=3N=C(SC3)C4=CC=CS4
InChIKey: KWJDHELCGJFUHW-SFTDATJTSA-N

Specifications

MW (average): 586.7030
Formula: C₂₆H₂₆N₄O₆S₃
CAS No.: 1008510-37-9
Physical state: Solid
Color: White to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO : 100 mg/mL

Documents

References

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

Same target

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Same research area

Search Inflammation/Immunology