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Lificiguat

Catalog No. T4381 CAS 170632-47-0

Synonyms: 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).

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Lificiguat, CAS 170632-47-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 61.00
25 mg	In stock	$ 127.00
50 mg	In stock	$ 252.00
100 mg	In stock	$ 432.00
200 mg	In stock	$ 639.00
500 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.92%

Purity: 99.48%

Purity: 98.85%

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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	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.
In vivo	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.
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.

Synonyms	YC-1
Molecular Weight	304.34
Formula	C19H16N2O2
CAS No.	170632-47-0

Storage

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

Solubility Information

DMSO: 30.4 mg/mL(100 mM)

References and Literature

1. Martin E,etal.YC-1 activation of human soluble guanylyl cyclase has both heme-dependent and heme-independent components.Proc Natl Acad Sci U S A. 2001 Nov 6;98(23):12938-42. 2. Yeo EJ,etal.YC-1: a potential anticancer drug targeting hypoxia-inducible factor 1.J Natl Cancer Inst. 2003 Apr 2;95(7):516-25.

Citations

1. Liu R, Kang Y, Chen L. Activation mechanism of human soluble guanylate cyclase by stimulators and activators. Nature Communications. 2021, 12(1): 1-10. 2. Li Y, Yang W, Zheng Y, et al.Targeting fatty acid synthase modulates sensitivity of hepatocellular carcinoma to sorafenib via ferroptosis.Journal of Experimental & Clinical Cancer Research.2023, 42(1): 1-19. 3. Liu X, Geng X, Shi Y, et al.Biomimetic oxygen-boosted hybrid membrane nanovesicles as the treatment strategy for ischemic stroke with the concept of the neurovascular unit.Biomaterials Advances.2023: 213379.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library GPCR Compound Library Bioactive Compounds Library Max Transcription Factor-Targeted Compound Library Glycometabolism Compound Library Glycolysis Compound Library HIF-1 Signaling Pathway Compound Library Glutamine Metabolism Compound Library Bioactive Compound Library NO PAINS Compound Library

Related Products

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Runcaciguat Glutaminyl Cyclase Inhibitor 1 Linaclotide Guanylin (mouse, rat) Methylene Blue BAY 41-2272 Nelociguat Praliciguat

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Keywords

Lificiguat 170632-47-0 Angiogenesis Chromatin/Epigenetic GPCR/G Protein Others Guanylate cyclase HIF Guanylate Cyclase Inhibitor YC 1 YC-1 YC1 inhibit inhibitor

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