Referencia número: HY-14927

Lificiguat

(Synonyms: YC-1)

36 Cited Publications

Revisión del cliente

Based on 36 publication(s) in Google Scholar

Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with K_d of 0.6-1.1 μM in the presence of CO.

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Pureza: 99.70%
No. CAS: 170632-47-0
Fòrmula: C₁₉H₁₆N₂O₂
Peso molecular:304.34

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Lificiguat Chemical Structure

No. CAS: 170632-47-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (36)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with K_d of 0.6-1.1 μM in the presence of CO.

IC₅₀ & Target

Kd: 0.6-1.1 μM (sGC, in the presence of CO)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	20.35 μM Compound: YC-1	Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay	[PMID: 33992863]
A2780	IC₅₀	80 μM Compound: YC-1	Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33992863]
A498	IC₅₀	0.3 μM Compound: YC-1	Cytotoxicity against human A498 cells incubated for 48 hrs by MTT assay Cytotoxicity against human A498 cells incubated for 48 hrs by MTT assay	[PMID: 26235951]
A498	IC₅₀	0.3 μM Compound: YC-1	Cytotoxicity against human A498 cells after 48 hrs by MTT assay Cytotoxicity against human A498 cells after 48 hrs by MTT assay	[PMID: 26820553]
A498	IC₅₀	0.37 μM Compound: YC-1	Cytotoxicity against human A498 cells after 48 hrs by MTT assay Cytotoxicity against human A498 cells after 48 hrs by MTT assay	[PMID: 23831809]
A549	IC₅₀	25.62 μM Compound: YC-1	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay	[PMID: 33992863]
A549	IC₅₀	80 μM Compound: YC-1	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33992863]
ACHN	IC₅₀	0.3 μM Compound: YC-1	Antitumor activity against human ACHN cells after 48 hrs by MTT assay Antitumor activity against human ACHN cells after 48 hrs by MTT assay	[PMID: 20097456]
AGS	IC₅₀	2 μM Compound: YC-1	Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay	[PMID: 17328532]
AGS	IC₅₀	2 μM Compound: YC-1	Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay	[PMID: 17884495]
HCT-116	IC₅₀	2.2 μM Compound: YC-1	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 24900662]
HEK293	IC₅₀	9.21 μM Compound: YC-1	Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay	[PMID: 19435661]
HeLa	IC₅₀	1.2 μM Compound: 1; YC-1	Inhibition of hypoxia-induced HIF1 transcriptional activity in human HeLa cells measured after 12 hrs by luciferase reporter gene assay Inhibition of hypoxia-induced HIF1 transcriptional activity in human HeLa cells measured after 12 hrs by luciferase reporter gene assay	[PMID: 27847273]
HeLa	IC₅₀	1.5 μM Compound: YC-1	Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay	[PMID: 24900662]
HeLa	IC₅₀	2 μM Compound: 12a, YC-1	Inhibition of HIF-1 (unknown origin) expressed in human HeLa cells after 12 hrs by HRE luciferase reporter gene assay Inhibition of HIF-1 (unknown origin) expressed in human HeLa cells after 12 hrs by HRE luciferase reporter gene assay	10.1039/C2MD20134H
HeLa	IC₅₀	2.4 μM Compound: YC-1	Inhibition of HIF1alpha transcriptional activity in human HeLa cells transfected with HRE-firefly luciferase and cytomegalovirus-promoter expressing Renilla luciferase incubated for 12 hrs under 1% O2 condition by dual luciferase reporter gene assay Inhibition of HIF1alpha transcriptional activity in human HeLa cells transfected with HRE-firefly luciferase and cytomegalovirus-promoter expressing Renilla luciferase incubated for 12 hrs under 1% O2 condition by dual luciferase reporter gene assay	[PMID: 31740202]
HeLa	IC₅₀	29.3 μM Compound: YC-1	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 24900662]
HeLa	IC₅₀	56 μM Compound: YC-1	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs under normoxia condition by MTT assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs under normoxia condition by MTT assay	[PMID: 31740202]
Hep 3B2	IC₅₀	13.8 μM Compound: YC-1	Inhibition of hypoxia induced HIF1 transcriptional activity in human Hep3B cells by cell-based HRE reporter assay Inhibition of hypoxia induced HIF1 transcriptional activity in human Hep3B cells by cell-based HRE reporter assay	[PMID: 17328532]
Hep 3B2	IC₅₀	13.8 μM Compound: YC-1	Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay	[PMID: 17884495]
HepG2	IC₅₀	2.2 μM Compound: YC-1	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 24900662]
HL-60	ED₅₀	25.27 μM Compound: YC-1	Cytotoxicity against HL60 cells by Propidium iodide exclusion assay Cytotoxicity against HL60 cells by Propidium iodide exclusion assay	[PMID: 17189698]
HL-60	IC₅₀	25.27 μM Compound: YC-1	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 23831809]
HL-60	IC₅₀	25.27 μM Compound: YC-1	Cytotoxicity against human HL60 cells incubated for 48 hrs by MTT assay Cytotoxicity against human HL60 cells incubated for 48 hrs by MTT assay	[PMID: 26235951]
HL-60	IC₅₀	25.3 μM Compound: YC-1	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 26820553]
HT-1080	IC₅₀	30.9 μM Compound: YC-1	Inhibition of cell proliferation of human HT1080 cells after 72 hrs by WST-8 dye based cell counting assay Inhibition of cell proliferation of human HT1080 cells after 72 hrs by WST-8 dye based cell counting assay	[PMID: 25773014]
HT-1080	IC₅₀	48.4 μM Compound: YC-1	Inhibition of HIF1 in human HT1080 cells transfected with 5xHRE/pGL3/VEGF/E1b reporter plasmid pre-incubated for 1 hr followed by incubation under hypoxia conditions for 24 hrs by HRE-driven luciferase reporter gene assay Inhibition of HIF1 in human HT1080 cells transfected with 5xHRE/pGL3/VEGF/E1b reporter plasmid pre-incubated for 1 hr followed by incubation under hypoxia conditions for 24 hrs by HRE-driven luciferase reporter gene assay	[PMID: 25773014]
L02	IC₅₀	26.58 μM Compound: YC-1	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay	[PMID: 33992863]
L02	IC₅₀	80 μM Compound: YC-1	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33992863]
MCF7	IC₅₀	80 μM Compound: YC-1	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33992863]
NCI-H226	IC₅₀	1.9 μM Compound: YC-1	Antitumor activity against human NCI-H226 cells after 48 hrs by MTT assay Antitumor activity against human NCI-H226 cells after 48 hrs by MTT assay	[PMID: 20097456]
Neutrophil	IC₅₀	>10 μM Compound: YC-1	Inhibition of fMLF/CB-induced human Neutrophil activation assessed as reduction in elastase release using MeO-Suc-Ala-Ala-Pro-Val-pnitroanilide as substrate incubated for 5 mins Inhibition of fMLF/CB-induced human Neutrophil activation assessed as reduction in elastase release using MeO-Suc-Ala-Ala-Pro-Val-pnitroanilide as substrate incubated for 5 mins	[PMID: 37918036]
Neutrophil	IC₅₀	>10 μM Compound: YC-1	Inhibition of fMLF/CB-induced human Neutrophil activation assessed as reduction in superoxide anion generation preincubated with compound for 2 mins prior to CB induction for 3 mins followed by fMLF addition by spectrophotometric analysis Inhibition of fMLF/CB-induced human Neutrophil activation assessed as reduction in superoxide anion generation preincubated with compound for 2 mins prior to CB induction for 3 mins followed by fMLF addition by spectrophotometric analysis	[PMID: 37918036]
PC-3	IC₅₀	>30 μM Compound: YC-1	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 24900662]
Platelet	IC₅₀	173 μM Compound: 1	Inhibition of thrombin-induced platelet aggregation in human platelet-rich plasma incubated for 1 min followed by thrombin addition Inhibition of thrombin-induced platelet aggregation in human platelet-rich plasma incubated for 1 min followed by thrombin addition	[PMID: 33049608]
Platelet	IC₅₀	53.8 μM Compound: 1	Inhibition of collagen-induced platelet aggregation in human platelet-rich plasma incubated for 1 min followed by collagen addition Inhibition of collagen-induced platelet aggregation in human platelet-rich plasma incubated for 1 min followed by collagen addition	[PMID: 33049608]
Platelet	IC₅₀	54.3 μM Compound: 1	Inhibition of arachidonic acid-induced platelet aggregation in human platelet-rich plasma incubated for 1 min followed by arachidonic acid addition Inhibition of arachidonic acid-induced platelet aggregation in human platelet-rich plasma incubated for 1 min followed by arachidonic acid addition	[PMID: 33049608]
Platelet	IC₅₀	87.3 μM Compound: 1	Inhibition of PAF-induced platelet aggregation in human platelet-rich plasma incubated for 1 min followed by PAF addition Inhibition of PAF-induced platelet aggregation in human platelet-rich plasma incubated for 1 min followed by PAF addition	[PMID: 33049608]
Sf21	EC₅₀	4.11 μM Compound: 2	Activation of sGC Enzyme (soluble Guanylate Cyclase) in Sf21 cells infected with baculo virus in the presence of 30 nM of PAPA/NO Activation of sGC Enzyme (soluble Guanylate Cyclase) in Sf21 cells infected with baculo virus in the presence of 30 nM of PAPA/NO	[PMID: 11141091]
SK-HEP1	IC₅₀	>30 μM Compound: YC-1	Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Sk-Hep1 cells by reporter gene assay Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Sk-Hep1 cells by reporter gene assay	[PMID: 17884495]

In Vitro

Soluble guanylate cyclase (sGC) is a heterodimeric heme protein and the primary NO receptor. Lificiguat (YC-1) binds near or directly to the heme-containing domain of the beta subunit. In the absence of CO, Lificiguat (YC-1) binds with K_d=9-21 μM, depending on construct. In the presence of CO, these values decrease to 0.6-1.1 μM. Lificiguat (YC-1) greatly enhanced CO binding to heterodimeric sGC, as expected (K_d=1 μM). Lificiguat (YC-1) stimulates sGC two- to four-fold in the absence of NO but acts synergistically with CO or NO to achieve several hundred fold activation. Binding of Lificiguat(YC-1) can also overcome inhibitory phosphorylation of sGC^[1]. Lificiguat (YC-1) is a soluble guanylyl cyclase (sGC) activator. HCC cell lines HepG2, BEL-7402 and HCCLM3 are incubated for 72 h with Sorafenib and/or Lificiguat (YC-1). Sorafenib or Lificiguat (YC-1) alone inhibits HCC cell proliferation in a dose-dependent manner. Moreover, combination of Sorafenib and Lificiguat (YC-1) significantly suppresses proliferation of HCC cells in a dose-dependent manner. In addition, at the ED₅₀ doses for both Sorafenib and Lificiguat (YC-1), combination index values (CI)=0.93 in HepG2, 0.95 in BEL-7402 and 0.72 in HCCLM3 respectively, suggesting that Sorafenib and Lificiguat (YC-1) synergistically inhibit proliferation of HCC cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Lificiguat (YC-1) (30 or 60 mg/kg, i.p.) inhibits MDA-MB-468 tumor growth in a dose-dependent manner. The effect of the prodrug formulation of Lificiguat (YC-1), YC-1-S, in MDA-MB-468 tumor-bearing mice is also investigated. In vivo pharmacokinetic analysis reveal that YC-1-S is quickly converted into its active form. Mice are administered 20, 40 or 80 mg/kg YC-1-S p.o. YC-1-S also displays dose-dependent inhibition of MDA-MB468 tumor growth. Both Lificiguat (YC-1) and YC-1-S dose-dependently reduce tumor weight. Moreover, the mean body weight of mice is not affected by Lificiguat (YC-1) or YC-1-S compare with vehicle-treated groups^[3]. Lificiguat (YC-1) is a potent NO-GC activator reported to improve rodent learning behavior when examined with the Morris water maze (MWM) and avoidance tests. Lificiguat (YC-1) enhances long-term potentiation (LTP) in hippocampal Schafer collateral-CA1 synapse via the NO-cGMP-PKG-dependent pathway and potentiated LTP induction in the amygdala, increases the activation of ERK, and potentiated the expression of brain-derived neurotrophic factor (BDNF) cAMP response element-binding protein (CREB) in response to fear memory test^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

No. CAS 170632-47-0
Appearance Solid
Peso molecular 304.34
Fòrmula C₁₉H₁₆N₂O₂
Color Off-white to yellow
SMILES

OCC1=CC=C(C2=NN(CC3=CC=CC=C3)C4=C2C=CC=C4)O1
Synonyms

YC-1
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (36)

All Cell Proliferation/Viability Assay2D/3D Cell Culture and DifferentiationCell Migration/Invasion AssayWBRT-PCRFlow CytometryCell Imaging/Staining

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Journal Impact Factor

Signal Transduct Target Ther

NOL7 facilitates melanoma progression and metastasis. [Abstract]

2021 Oct 13;6(1):352. PMID: 34642294
Adv Sci (Weinh)

Targeted SPP1 Inhibition of Tumor-Associated Myeloid Cells Effectively Decreases Tumor Sizes. [Abstract]

2024 Dec 5:e2410360. PMID: 39639496
Research (Wash D C)

Trabecular-Like Scaffold Dictates Osteogenesis via Fluid Shear Stress-Induced Metabolic Reprogramming through the CAV1-HIF-1α Axis. [Abstract]

2026 Jun 16:9:1307. PMID: 42312216
Cell Death Dis

Oncometabolite fumarate facilitates PD-L1 expression and immune evasion in clear cell renal cell carcinoma. [Abstract]

2025 Jun 3;16(1):432. PMID: 40461489

Lificiguat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Jun 3;16(1):432. [Abstract]

YC-1 (5 μM, 48 h) inhibits DMF/FHIN1-mediated upregulation of PD-L1 in ccRCC cells.

Lificiguat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Jun 3;16(1):432. [Abstract]

YC-1 (5 μM, 48 h) inhibits DMF/FHIN1-mediated upregulation of PD-L1 in ccRCC cells.

Lificiguat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Jun 3;16(1):432. [Abstract]

YC-1 (5 μM, 48 h) reduced DMF-induced upregulation of PD-L1 levels on tumor cell surfaces.

Lificiguat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Jun 3;16(1):432. [Abstract]

After pre-treatment with or without YC-1 (5 μM，12 h), CCS1477, or PKM2-IN-1, DMF-treated RCC4 cells were cocultured with activated T cells for 48 h, followed by crystal violet staining. The quantification is shown on the right.
Cell Death Dis

SIRT6 promotes angiogenesis and hemorrhage of carotid plaque via regulating HIF-1α and reactive oxygen species. [Abstract]

2021 Jan 12;12(1):77. PMID: 33436551

Lificiguat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Jan 12;12(1):77. [Abstract]

Cell proliferation of HUVECs-NC, HUVECs-SIRT6, and HUVECs-SIRT6 treated with HIF-1α inhibitor YC-1 (1 μm for 0-72 h) under both hypoxia and normoxia, performed by CCK8 assays.

Lificiguat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Jan 12;12(1):77. [Abstract]

Tube formation ability of HUVECs-NC, HUVECs-SIRT6, and HUVECs-SIRT6 pre-treated with HIF-1α inhibitor YC-1 (1 μm for 24 h) under both hypoxia and normoxia (magnification: ×200).

Lificiguat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Jan 12;12(1):77. [Abstract]

Invasion and migration ability of HUVECs-NC, HUVECs-SIRT6, and HUVECs-SIRT6 treated with HIF-1α inhibitor YC-1 (1 μm for 24 h) under both hypoxia and normoxia, performed by transwell assays (magnification: ×400).

Lificiguat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Jan 12;12(1):77. [Abstract]

Migration ability of HUVECs-NC, HUVECs-SIRT6, and HUVECs-SIRT6 treated with HIF-1α inhibitor YC-1 (1 μm for 24 h) under both hypoxia and normoxia, performed by wound healing assay (magnification: ×100).
Adv Healthc Mater

Spatiotemporal regulation of injectable heterogeneous silk gel scaffolds for accelerating guided vertebral repair. [Abstract]

2023 Mar;12(7):e2202210. PMID: 36465008
J Transl Med

HIF-1α-mediated LAMC1 overexpression is an unfavorable predictor of prognosis for glioma patients: evidence from pan-cancer analysis and validation experiments. [Abstract]

2024 Apr 27;22(1):391. PMID: 38678297
J Transl Med

Chemotherapy induces ACE2 expression in breast cancer via the ROS-AKT-HIF-1α signaling pathway: a potential prognostic marker for breast cancer patients receiving chemotherapy. [Abstract]

2022 Nov 5;20(1):509. PMID: 36335375
Int J Nanomedicine

ROS-Responsive Nanosystem Targeted Co-Delivery YC-1 and Regorafenib to Alleviate Hypoxia Enhancing Hepatocellular Carcinoma Therapy. [Abstract]

2025 Jul 1:20:8481-8496. PMID: 40620686
Antioxidants (Basel)

Hypoxia Aggravates Neuron Ferroptosis in Early Brain Injury Following Subarachnoid Hemorrhage via NCOA4-Meditated Ferritinophagy. [Abstract]

2023 Dec 11;12(12):2097. PMID: 38136217
Stem Cell Res Ther

Prostaglandin E1 reduces apoptosis and improves the homing of mesenchymal stem cells in pulmonary arterial hypertension by regulating hypoxia-inducible factor 1 alpha. [Abstract]

2022 Jul 16;13(1):316. PMID: 35842683
J Ethnopharmacol

Exploration of the underlying mechanism of Astragaloside III in attenuating immunosuppression via network pharmacology and vitro/vivo pharmacological validation. [Abstract]

2024 Aug 10:330:118235. PMID: 38648891
J Ethnopharmacol

Systems pharmacology reveals the mechanism of Astragaloside IV in improving immune activity on cyclophosphamide-induced immunosuppressed mice. [Abstract]

2023 Sep 15:313:116533. PMID: 37100262
Ecotoxicol Environ Saf

HMGA2/PHGDH axis-mediated glycolysis under hypoxia is required for cadmium-induced A549 cell migration. [Abstract]

2025 Aug 4:303:118787. PMID: 40763516
Int Immunopharmacol

TAMs-derived SPP1, regulated by HIF-1α/STAT3 signaling pathway, influences colorectal cancer malignant progression by activation of EMT via integrin αvβ3. [Abstract]

2025 May 26:159:114947. PMID: 40424660
Int J Mol Sci

HIF-1α Negatively Regulates Irisin Expression Which Involves in Muscle Atrophy Induced by Hypoxia. [Abstract]

2022 Jan 14;23(2):887. PMID: 35055073
Sci Rep

Taurine stimulates EPO production in feline renal cells through the HIF pathway. [Abstract]

2026 Apr 9;16(1):16713. PMID: 41957466
Food Qual Saf

2025 Aug 4.
Sci Rep

Investigating the mechanism of Gentiopicroside in rheumatoid arthritis through network pharmacology, molecular docking, and experimental validation. [Abstract]

2025 Jun 6;15(1):19871. PMID: 40473698
J Virol

PTBP1 is upregulated in response to Zika virus infection and restrains viral replication by hijacking viral NS1 protein to induce NS1 degradation. [Abstract]

2026 Apr 27:e0149525. PMID: 42037413
Cell Stress Chaperones

HSPA12A stimulates "Smurf1-Hif1α-aerobic glycolysis" axis to promote proliferation of renal tubular epithelial cells after hypoxia/reoxygenation injury. [Abstract]

2024 Oct;29(5):681-695. PMID: 39349238
J Infect Dis

Impact of Hypoxia-Inducible Factor-1α on Host Immune Metabolism and Tissue Damage During Mycobacterium bovis Infection. [Abstract]

2024 Jun 6:jiae305. PMID: 38843067
BMC Cancer

β2AR-HIF-1α-CXCL12 signaling of osteoblasts activated by isoproterenol promotes migration and invasion of prostate cancer cells. [Abstract]

2019 Nov 26;19(1):1142. PMID: 31771535
J Neurotrauma

Stabilization of Hypoxia Inducible Factor-1α by Dimethyloxalylglycine Promotes Recovery from Acute Spinal Cord Injury by Inhibiting Neural Apoptosis and Enhancing Axon Regeneration. [Abstract]

2019 Dec 15;36(24):3394-3409. PMID: 31232175
Tuberculosis

Activation of hypoxia-inducible factor 1 (Hif-1) enhanced bactericidal effects of macrophages to Mycobacterium tuberculosis. [Abstract]

2021 Jan:126:102044. PMID: 33383382
Radiat Environ Biophys

Hypoxia inducible factor-1α/B-cell lymphoma 2 signaling impacts radiosensitivity of H1299 non-small cell lung cancer cells in a normoxic environment. [Abstract]

2019 Aug;58(3):439-448. PMID: 31203382

Lificiguat purchased from MedChemExpress. Usage Cited in: Radiat Environ Biophys. 2019 Aug;58(3):439-448. [Abstract]

Western blot analysis reveals HIF-1α and BCL-2 expression in the four types of H1299 cells exposed to radiation following YC-1 pretreatment. β-actin level is determined as internal control.
Biochem Cell Biol

VEGF-mediated angiogenesis in retinopathy of prematurity is co-regulated by miR-17-5p and miR-20a-5p. [Abstract]

2021 Aug;99(4):414-423. PMID: 34319836
Hum Mutat

Albiflorin-Mediated MAP2K1 Targeting and HIF-1 Signaling Inhibition Contribute to the Therapeutic Efficacy in Hyperuricemia-Associated Cognitive Impairment. [Abstract]

2026 Jan 19:2026:5859468. PMID: 41561638
bioRxiv

2024 November 19.
Res Sq

2024 Jul 15.
Biomed Pharmacother

Chrysin inhibits ferroptosis of cerebral ischemia/reperfusion injury via regulating HIF-1α/CP loop. [Abstract]

2024 May:174:116500. PMID: 38555815
Research Square Preprint

2024 Jan 11.
bioRxiv

2023 Jan 30.
Aging

Bnip3 interacts with vimentin, an intermediate filament protein, and regulates autophagy of hepatic stellate cells. [Abstract]

2020 Dec 3;13(1):957-972. PMID: 33290258
Research Square Preprint

2020 Oct.
Biomed Pharmacother

Safflower yellow promotes angiogenesis through p-VHL/ HIF-1α/VEGF signaling pathway in the process of osteogenic differentiation. [Abstract]

2018 Nov:107:1736-1743. PMID: 30257392

Lificiguat purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Nov:107:1736-1743. [Abstract]

Western blot is used to assess the protein levels of VEGF, Ang-2, ALP, Runx2, and OPN-1 in the co-culture of HUVEC-12 and BMSCs. β-actin is used as a loading control.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (328.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2858 mL

16.4290 mL

32.8580 mL

5 mM

0.6572 mL

3.2858 mL

6.5716 mL

10 mM

0.3286 mL

1.6429 mL

3.2858 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (8.21 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocolo

Kinase Assay^[1]

CO dissociation constants are measured by titrating CO from a saturated solution into sGC protein and monitoring the appearance of the CO-bound Soret absorption band. The Ms sGC β₁(1-380) and Bt sGC β₁(1-197) samples are prepared in Ar-purged buffer supplemented with excess dithionite. CO binding experiments are performed in a 10 cm pathlength cuvette for Ms sGC-β₁(1-380) and Ms sGC-NT21 using a Cary 50 spectrophotometer with a modified sample holder. Binding data in the presence and absence of 50 μM Lificiguat (YC-1) is plotted using a single site saturation ligand binding model in SigmaPlot^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[2]

Cell proliferation assay is measured using a Cell Counting Kit-8 (CCK-8). Briefly, cells are cultured in 96-well plates at a concentration of 3×10³/well, incubated for 24 h, and treated with Sorafenib and/or Lificiguat (YC-1). After 72 h treatment, CCK-8 reagent is added to each well. The absorbance is measured at 450 nm after 2.5 h incubation at 37°C using an automated ELISA plate reader. Any synergistic effects resulting from combination of the compounds are measured using Microsoft Excel software to determine the combination index values (CI>1: antagonistic effect, CI=1: additive effect, and CT<1: synergistic effect)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]^[4]

Mice^[3]
Fifty-eight female nu/nu mice (4 weeks-old) are used. MDA-MB-468 breast cancer cells (5×10⁶ cells per mouse) are suspended in 0.1 mL of Matrigel solution (50% v/v Matrigel in PBS) and inoculated into the mammary fat pads of nude mice. When the tumor masses reach 100 mm³, the tumor-bearing mice are randomly divided into groups for treatments with different Lificiguat (YC-1)/YC-1-S doses. The mice are i.p. injected with YC-1 (30 or 60 mg/kg) or administered YC-1-S p.o. Tumor size and mouse body weight are measured once every 3 days, and tumor volume (mm³) is calculated using the equation: length×(width)²×0.5. At the end of the experiments, mice are killed and tumor nodules are dissected and weighed. Tumor tissues are subjected to Western blotting.
Rats^[4]
4-month-old (200-250 g) and 24-month-old (550-600 g) male Wistar-albino rats are used. Lificiguat (YC-1) is prepared immediately prior to use and given intraperitoneally (i.p.) in a volume of 0.1 mL per 100 g body weight. All rats receives 1 mg/kg/day of Lificiguat (YC-1) for 2 weeks. DMSO is administered to 4-month-old and 24-month-old rats (n=10, for each group). Doses are selected to confirm the selected doses on locomotor activity; all results are measured.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (289 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Purohit R, et al. YC-1 binding to the β subunit of soluble guanylyl cyclase overcomes allosteric inhibition by the α subunit. Biochemistry. 2014 Jan 14;53(1):101-14. [Content Brief]

[2]. Kong J, et al. YC-1 enhances the anti-tumor activity of sorafenib through inhibition of signal transducer and activator of transcription 3 (STAT3) in hepatocellular carcinoma. Mol Cancer. 2014 Jan 13;13:7. [Content Brief]

[3]. Chang LC, et al. YC-1 inhibits proliferation of breast cancer cells by down-regulating EZH2 expression via activation of c-Cbl and ERK. Br J Pharmacol. 2014 Sep;171(17):4010-25. [Content Brief]

[4]. Komsuoglu Celikyurt I, et al. Effects of YC-1 on Learning and Memory Functions of Aged Rats. Med Sci Monit Basic Res. 2014 Aug 21;20:130-7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2858 mL	16.4290 mL	32.8580 mL	82.1450 mL
	5 mM	0.6572 mL	3.2858 mL	6.5716 mL	16.4290 mL
	10 mM	0.3286 mL	1.6429 mL	3.2858 mL	8.2145 mL
	15 mM	0.2191 mL	1.0953 mL	2.1905 mL	5.4763 mL
	20 mM	0.1643 mL	0.8214 mL	1.6429 mL	4.1072 mL
	25 mM	0.1314 mL	0.6572 mL	1.3143 mL	3.2858 mL
	30 mM	0.1095 mL	0.5476 mL	1.0953 mL	2.7382 mL
	40 mM	0.0821 mL	0.4107 mL	0.8214 mL	2.0536 mL
	50 mM	0.0657 mL	0.3286 mL	0.6572 mL	1.6429 mL
	60 mM	0.0548 mL	0.2738 mL	0.5476 mL	1.3691 mL
	80 mM	0.0411 mL	0.2054 mL	0.4107 mL	1.0268 mL
	100 mM	0.0329 mL	0.1643 mL	0.3286 mL	0.8214 mL

Keywords

Lificiguat

36 Cited Publications

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Lificiguat

GPCR/G Protein Compound Library

Anti-Cancer Compound Library

Anti-Cardiovascular Disease Compound Library

Targeted Diversity Library

Human Metabolite Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Lificiguat

Actividad biológica

Chemical Information

Publications (36)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Lificiguat

GPCR/G Protein Compound Library

Anti-Cancer Compound Library

Anti-Cardiovascular Disease Compound Library

Targeted Diversity Library

Human Metabolite Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Lificiguat

Actividad biológica

Chemical Information

Publications (36)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Lificiguat Related Classifications

HY-14927 Related Classifications