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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Protein Phosphatase/PTP-AKB-9778
AKB-9778

Chemical Structure : AKB-9778

CAS No.: 1008510-37-9

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AKB-9778 (Razuprotafib, AKB9778)

货号: PC-61676Not For Human Use, Lab Use Only.

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

规格 价格 库存 数量
2 mg ￥2580 In stock
5 mg ￥4280 In stock
10 mg ￥7280 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AKB-9778 (Razuprotafib) 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.

物理化学性质&存储条件

分子量 586.70
分子式 C26H26N4O6S3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(4-((S)-2-((S)-2-((methoxycarbonyl)amino)-3-phenylpropanamido)-2-(2-(thiophen-2-yl)thiazol-4-yl)ethyl)phenyl)sulfamic acid

参考文献

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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