Lificiguat (YC-1)

Catalog No.S7958

For research use only.

Lificiguat (YC-1) is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha).

Lificiguat (YC-1) Chemical Structure

CAS No. 170632-47-0

Selleck's Lificiguat (YC-1) has been cited by 22 publications

Purity & Quality Control

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Biological Activity

Description Lificiguat (YC-1) is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha).
Targets
sGC [1] HIF-1α [2]
In vitro

YC-1 is an allosteric activator of soluble guanylyl cyclase (sGC). YC-1 increases the catalytic rate of the enzyme 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 [1]. 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[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Assay
Methods Test Index PMID
Western blot DNMT1 / DNMT3a / DNMT3b ; EZH2 / EZH1 / H3K27me3 / Histone H3 ; p-ERK / p-p38 MAPK / p-JNK1 / p-AKT ; HIF-1α ; HO-1 / HO-2 24697523 18923065 22507221
Growth inhibition assay Cell viability ; Cell proliferation 22507221
In vivo The administration of YC-1 to experimental animals results in the inhibition of the platelet-rich thrombosis and a decrease of the mean arterial pressure, which correlates with increased cGMP levels [1]. YC-1 effectively inhibits tumor growth in tumor-bearing mice. The inhibition of HIF-1 activity in tumors from YC-1-treated mice 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 growt[2].

Protocol (from reference)

Cell Research:[2]
  • Cell lines: Hep3B cells
  • Concentrations: 0.01-10 μM
  • Incubation Time: 24 h
  • Method: 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.
Animal Research:[2]
  • Animal Models: Male nude (BALB/cAnNCrj–nu/nu) mice
  • Dosages: 30 µg/g
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 304.34
Formula

C19H16N2O2

CAS No. 170632-47-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=N2)C4=CC=C(O4)CO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO % % Tween 80 % ddH2O
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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