Lificiguat (YC-1)

Catalog No.S7958 Batch:S795801

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Technical Data

Formula

C19H16N2O2
Molecular Weight 304.34 CAS No. 170632-47-0
Solubility (25°C)* In vitro DMSO 60 mg/mL (197.14 mM)
Ethanol 60 mg/mL (197.14 mM)
Water Insoluble
* <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.)

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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].
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.

Selleck's Lificiguat (YC-1) has been cited by 33 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
Hypoxia enhances autophagy level of human sperms [ Sci Rep, 2024, 14(1):8465] PubMed: 38605082
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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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