1. GPCR/G Protein
  2. Guanylate Cyclase

Lificiguat (Synonyms: YC-1)

Cat. No.: HY-14927 Purity: 99.19%
Handling Instructions

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

For research use only. We do not sell to patients.
Lificiguat Chemical Structure

Lificiguat Chemical Structure

CAS No. : 170632-47-0

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 77 In-stock
5 mg USD 70 In-stock
10 mg USD 125 In-stock
50 mg USD 546 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with Kd 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]

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 Kd=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 (Kd=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].

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].

Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
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.
Kinase Assay

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

Cell Assay

Lificiguat (YC-1) is dissolved in DMSO and stored, and then diluted with appropriate media before use[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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

Lificiguat (YC-1) is dissolved in DMSO and diluted with saline[3][4].

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

Molecular Weight








Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 51 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.19%

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