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Lificiguat

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Catalog No. T4381Cas No. 170632-47-0
Alias YC-1

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

Lificiguat

🥰Excellent
Purity: 99.92%
Catalog No. T4381Alias YC-1Cas No. 170632-47-0
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).
Pack SizePriceAvailabilityQuantity
5 mg$43In Stock
10 mg$61In Stock
25 mg$127In Stock
50 mg$252In Stock
100 mg$432In Stock
200 mg$639In Stock
500 mg$987In Stock
1 mL x 10 mM (in DMSO)$48In Stock
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Purity:99.92%
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Product Introduction

Bioactivity
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&IC50
sGC (presence of CO):0.6-1.1 μM (Kd)
In vitro
Lificiguat increases the catalytic rate of the soluble guanylyl cyclase (sGC) and sensitizes the enzyme toward its gaseous activators nitric oxide or carbon monoxide. Lificiguat 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. Lificiguat 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 Lificiguat are likely to be linked with the oxygen-sensing pathway and not with the activation of soluble guanylyl cyclase.
In vivo
In experimental animals, Lificiguat causes the inhibition of the platelet-rich thrombosis and a decrease of the mean arterial pressure. Lificiguat effectively inhibits tumor growth in tumor-bearing mice. In mice, Lificiguat 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 Lificiguat does not appear to affect tumor growth.
Cell Research
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
Animal Models: Male nude (BALB/cAnNCrj–nu/nu) mice. Formulation: DMSO. Dosages: 30 μg/g. Administration: i.p.
AliasYC-1
Chemical Properties
Molecular Weight304.34
FormulaC19H16N2O2
Cas No.170632-47-0
SmilesOCc1ccc(o1)-c1nn(Cc2ccccc2)c2ccccc12
Relative Density.1.24 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 70 mg/mL (230.01 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.2858 mL16.4290 mL32.8580 mL164.2899 mL
5 mM0.6572 mL3.2858 mL6.5716 mL32.8580 mL
10 mM0.3286 mL1.6429 mL3.2858 mL16.4290 mL
20 mM0.1643 mL0.8214 mL1.6429 mL8.2145 mL
50 mM0.0657 mL0.3286 mL0.6572 mL3.2858 mL
100 mM0.0329 mL0.1643 mL0.3286 mL1.6429 mL

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