Razuprotafib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Razuprotafib (AKB-9778) 是一种有效的选择性 VE-PTP（血管内皮蛋白酪氨酸磷酸酶）催化活性抑制剂，IC50 为 17 pM。

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).

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

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

AKB-9778

Metabolic Enzyme/Protease

Phosphatase

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1008510-37-9

586.7

C??H??N?O?S?

>98% (HPLC)

DMSO : 100 mg/mL (170.44 mM; Need ultrasonic)

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

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(-20℃)

With Ice Pack

≥ 2 years