| Bioactivity | Norleual TFA, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC50 of 3 pM. Norleual TFA is an AT4 receptor antagonist and exhibits potent antiangiogenic activities[1]. | ||||||
| Invitro | Norleual TFA（20 和 50 pM）显着降低 HGF 依赖性 c-Met 和 Gab1 磷酸化。20 pM Norleual TFA 显着降低 HEK293 细胞中 HGF 启动的 Gab1 和 c-Met 之间的关联。Norleual TFA 显着减弱 HGF 依赖性 c-Met 激活和下游信号[1]。Norleual TFA（1 pM-1 μM；4 天）能够在 MDCK 细胞中以皮摩尔范围内的浓度抑制多种细胞类型中的 HGF 依赖性信号转导、增殖、迁移和侵袭[1]。 | ||||||
| In Vivo | Norleual TFA（50 μg/kg；腹腔注射；每天 1 次，持续 2 周；C57BL/6 小鼠）抑制 B16-F10 小鼠黑色素瘤细胞在肺部的定植[1]。 | ||||||
| Name | Norleual TFA | ||||||
| Formula | C43H59F3N8O9 | ||||||
| Molar Mass | 888.97 | ||||||
| Appearance | Solid | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage | Sealed storage, away from moisture and light, under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen) |
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| Reference | [1]. B J Yamamoto, et al. The angiotensin IV analog Nle-Tyr-Leu-psi-(CH2-NH2)3-4-His-Pro-Phe (norleual) can act as a hepatocyte growth factor/c-Met inhibitor. J Pharmacol Exp Ther. 2010 Apr;333(1):161-73. |