Lificiguat (YC-1)

Catalog No.S7958 Batch:S795804

Technical Data

Formula

C₁₉H₁₆N₂O₂

Molecular Weight

304.34

CAS No.

170632-47-0

Solubility (25°C)*

In vitro

DMSO

61 mg/mL (200.43 mM)

Ethanol

61 mg/mL (200.43 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.51mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 10.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.05mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 61 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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].

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 Assay:^{^[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 Study:^{^[2]}	Animal Models Male nude (BALB/cAnNCrj–nu/nu) mice Dosages 30 µg/g Administration i.p.

Cell Assay:^{^[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 Study:^{^[2]}

Animal Models
Male nude (BALB/cAnNCrj–nu/nu) mice
Dosages
30 µg/g
Administration
i.p.

References

Selleck's Lificiguat (YC-1) has been cited by 32 publications

Inhibition of OGFOD1 by FG4592 confers neuroprotection by activating unfolded protein response and autophagy after ischemic stroke [ J Transl Med, 2024, 22(1):248]	PubMed: 38454480
Aging aggravates liver fibrosis through downregulated hepatocyte SIRT1-induced liver sinusoidal endothelial cell dysfunction [ Hepatol Commun, 2024, 8(1)e0350]	PubMed: 38126919
Bioinformatics integration reveals key genes associated with mitophagy in myocardial ischemia-reperfusion injury [ BMC Cardiovasc Disord, 2024, 24(1):183]	PubMed: 38539069
Zinc oxide nanoparticles inhibit osteosarcoma metastasis by downregulating β-catenin via HIF-1α/BNIP3/LC3B-mediated mitophagy pathway [ Bioact Mater, 2023, 19:690-702]	PubMed: 35600978
Stellate ganglion block ameliorated central post-stroke pain with comorbid anxiety and depression through inhibiting HIF-1α/NLRP3 signaling following thalamic hemorrhagic stroke [ J Neuroinflammation, 2023, 20(1):82]	PubMed: 36944982
Lactate modulates microglial inflammatory responses after oxygen-glucose deprivation through HIF-1α-mediated inhibition of NF-κB [ Brain Res Bull, 2023, S0361-9230(23)00033-3]	PubMed: 36746287
[HIF-1α activation induces cholesterol homeostasis dysfunction to accelerate progression of diabetic nephropathy in rats] [ Nan Fang Yi Ke Da Xue Xue Bao, 2023, 43(10):1782-1788]	PubMed: 37933655
Notch-triggered maladaptation of liver sinusoidal endothelium aggravates nonalcoholic steatohepatitis through eNOS [ Hepatology, 2022, 10.1002/hep.32332]	PubMed: 35006626
PD-1+ CD4 T cell immune response is mediated by HIF-1α/NFATc1 pathway after P. yoelii infection [ Front Immunol, 2022, 13:942862]	PubMed: 36091043
PD-1+ CD4 T cell immune response is mediated by HIF-1α/NFATc1 pathway after P. yoelii infection [ Front Immunol, 2022, 13:942862]	PubMed: 36091043

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SHIPPING AND STORAGE
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