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EG00229
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EG00229图片
CAS NO:1210945-69-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
EG00229 是一种神经纤毛蛋白 1 (NRP1) 受体拮抗剂。 EG00229 选择性抑制 VEGF-A 与 NRP1 b1 结构域的结合,IC50 为 3 μM,但对 VEGFA 与 VEGFR-1 和 VEGFR-2 的结合没有影响。
Cas No.1210945-69-9
化学名(S,Z)-2-(((3-(benzo[c][1,2,5]thiadiazole-4-sulfonamido)thiophen-2-yl)(hydroxy)methylene)amino)-5-guanidinopentanoic acid compound with 2,2,2-trifluoroacetic acid (1:1)
Canonical SMILESN=C(NCCC[C@@](/N=C(O)/C1=C(NS(C2=CC=CC3=NSN=C32)(=O)=O)C=CS1)([H])C(O)=O)N.FC(F)(F)C(O)=O
分子式C19H20F3N7O7S3
分子量611.6
溶解度Soluble in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

EG00229 is a small molecule inhibitor of neuropilin-1(Nrp1) with an IC50 of 3μM [1].

EG00229 has been reported to inhibit VEGF-A binding to PAE/NRP1 in the Nrp1and bt-VEGF-A binding to purified Nrp1 b1 domain in a cell-free assay with an IC50 value of 8μM and 3μM, respectively. In addition, EG00229 has also shown the inhibition of VEGF-A binding to VEGFR2, VEGFR1 and Nrp1 in human umbilical vein endothelial cells (HUVECs) in a dose-dependent manner with an IC50 value of 23μM [1]. Besides, EG00229 has been revealed to prevent tuftsin binding to the Nrp1 which is at the cell surface. Moreover, EG00229 has been noted to suppress the anti-inflammatory M2 shift in microglia induced by tuftsin and thus potently prevent tuftsin’s action [2].

References:
[1] Jarvis A1, Allerston CK, Jia H, Herzog B, Garza-Garcia A, Winfield N, Ellard K, Aqil R, Lynch R, Chapman C, Hartzoulakis B, Nally J, Stewart M, Cheng L, Menon M, Tickner M, Djordjevic S, Driscoll PC, Zachary I, Selwood DL.Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction. J Med Chem. 2010 Mar 11;53(5):2215-26.
[2] Nissen JC1, Selwood DL, Tsirka SE. Tuftsin signals through its receptor neuropilin-1 via the transforming growth factor beta pathway. J Neurochem. 2013 Nov;127(3):394-402.