利非西呱 T4381

Product Introduction
Bioactivity


英文名: Lificiguat

描述: Lificiguat (YC-1) 是一种不依赖一氧化氮的可溶性鸟苷酸环化酶激活剂和低氧诱导因子 1α 的抑制剂。

细胞实验: Hep3B cells are plated in a six-well plate at a density of 1 × 105 cells/well in α-modified Eagle medium supplemented with 10% heat-inactivated FBS and incubated overnight. Cells are treated with YC-1 (0.01-10 μM) or vehicle (DMSO) for 5 minutes and are then subjected to normoxia or hypoxia for 24 hours. VEGF levels in the conditioned media are quantified by using the Quantikine human VEGF Immunoassay kit. The VEGF concentrations are quantified by comparison with a series of VEGF standard samples included in the assay kit.

动物实验: Animal Models: Male nude (BALB/cAnNCrj–nu/nu) mice. Formulation: DMSO. Dosages: 30 μg/g. Administration: i.p.

体外活性: YC-1 increases the catalytic rate of the soluble guanylyl cyclase (sGC) and sensitizes the enzyme toward its gaseous activators nitric oxide or carbon monoxide. YC-1 alone activates the enzyme only 10-fold, but it potentiates the CO- and NO-dependent activation of sGC, resulting in stimulation of the highly purified enzyme that may be several hundred- to several thousand-fold. It inhibits platelet aggregation and vascular contraction and also inhibits HIF-1 activity in vitro. YC-1 completely blocks HIF-1α expression at the post-transcriptional level and consequently inhibits the transcription factor activity of HIF-1 in hepatoma cells cultured under hypoxic conditions, suggesting that these effects of YC-1 are likely to be linked with the oxygen-sensing pathway and not with the activation of soluble guanylyl cyclase.

体内活性: In experimental animals, YC-1 causes the inhibition of the platelet-rich thrombosis and a decrease of the mean arterial pressure. YC-1 effectively inhibits tumor growth in tumor-bearing mice. In mice, YC-1 inhibition of HIF-1 activity in tumors, and this is associated with blocked angiogenesis and an inhibition of tumor growth, while the anti-platelet aggregation effect of YC-1 does not appear to affect tumor growth.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 30.4 mg/mL(100 mM)


关键字: Guanylate Cyclase | Lificiguat | Inhibitor | YC 1 | YC1 | inhibit

相关产品: Vericiguat | Nitroprusside disodium dihydrate | Guanylin (mouse, rat) | Glutaminyl Cyclase Inhibitor 1 | Olinciguat | Methylene Blue trihydrate | Runcaciguat | Uroguanylin (human) | Plecanatide | Nelociguat

相关库: HIF-1 Signaling Pathway Compound Library | Glycometabolism Compound Library | Bioactive Lipid Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | GPCR Compound Library | Anti-Pancreatic Cancer Compound Library | Preclinical Compound Library | Reprogramming Compound Library | Bioactive Compound Library

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