[CAS NO. 170632-47-0] Lificiguat

Name: Lificiguat
Brand: Arctom Scientific
SKU: AS721069

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PRODUCTS SPECIFICATIONS [170632-47-0]

Fulfillment

Catalog

AS721069

Brand

Arctom Scientific

CAS

170632-47-0

DESCRIPTION [170632-47-0]

Overview

MDL	MFCD06407798
Molecular Weight	304.34
Molecular Formula	C19H16N2O2
SMILES	OCC1=CC=C(C2=NN(CC3=CC=CC=C3)C4=C2C=CC=C4)O1

For research use only. We do not sell to patients.

15 Publications Citing Use of MCE

Summary

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]

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 ED ₅₀ 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] .

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] .

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

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 328.58 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent 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.

In Vivo:

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
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
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.

References

Synonyms

2-Furanmethanol, 5-[1-(phenylmethyl)-1H-indazol-3-yl]-

5-[1-(Phenylmethyl)-1H-indazol-3-yl]-2-furanmethanol

YC 1

YC 1 (pharmaceutical)

1-Benzyl-3-(5-hydroxymethylfur-2-yl)indazole

Lificiguat

1-Benzyl-3-(5-hydroxymethyl-furan-2-yl)indazole

[5-(1-Benzyl-1H-indazol-3-yl)-furan-2-yl]-methanol

[5-(1-Benzylindazol-3-yl)furan-2-yl]methanol