Lificiguat (YC-1)

製品コード：S7958 純度：99.94%

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).

CAS No. 170632-47-0

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 59500	国内在庫あり
200mg	JPY 149500	国内在庫あり
1g	JPY 448500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（32）

製品安全説明書

現在のバッチを見る：純度： 99.94%

99.94

Lificiguat (YC-1)関連製品

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シグナル伝達経路

HIFシグナル伝達経路

HIF阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HT60	Apoptosis assay	26 uM	48 hrs	Induction of apoptosis in HT60 cells at 26 uM after 48 hrs	17189698
HeLa	Function assay	30 uM	4 hrs	Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot	19435661
HCT116	Function assay	30 uM	4 hrs	Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot	19435661
HCT116	Function assay	3 uM		Reduction of insulin-induced HIF-1 alpha expression in human HCT116 cells at 3 uM by western blot analysis	27157007
HEK293	Function assay		16 hrs	Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay, IC50 = 9.21 μM.	19435661
ACHN	Antitumor assay		48 hrs	Antitumor activity against human ACHN cells after 48 hrs by MTT assay, IC50 = 0.3 μM.	20097456
NCI-H226	Antitumor assay		48 hrs	Antitumor activity against human NCI-H226 cells after 48 hrs by MTT assay, IC50 = 1.9 μM.	20097456
A498	Cytotoxicity assay		48 hrs	Cytotoxicity against human A498 cells after 48 hrs by MTT assay, IC50 = 0.37 μM.	23831809
HL60	Cytotoxicity assay		48 hrs	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, IC50 = 25.27 μM.	23831809
HeLa	Function assay		12 hrs	Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay, IC50 = 1.5 μM.	24900662
HepG2	Cytotoxicity assay		72 hrs	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 2.2 μM.	24900662
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 2.2 μM.	24900662
HeLa	Cytotoxicity assay		72 hrs	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50 = 29.3 μM.	24900662
HT1080	Proliferation assay		72 hrs	Inhibition of cell proliferation of human HT1080 cells after 72 hrs by WST-8 dye based cell counting assay, IC50 = 30.9 μM.	25773014
HT1080	Function assay		1 hr	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, IC50 = 48.4 μM.	25773014
A498	Cytotoxicity assay		48 hrs	Cytotoxicity against human A498 cells incubated for 48 hrs by MTT assay, IC50 = 0.3 μM.	26235951
HL60	Cytotoxicity assay		48 hrs	Cytotoxicity against human HL60 cells incubated for 48 hrs by MTT assay, IC50 = 25.27 μM.	26235951
A498	Cytotoxicity assay		48 hrs	Cytotoxicity against human A498 cells after 48 hrs by MTT assay, IC50 = 0.3 μM.	26820553
HL60	Cytotoxicity assay		48 hrs	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, IC50 = 25.3 μM.	26820553
HeLa	Function assay		12 hrs	Inhibition of hypoxia-induced HIF1 transcriptional activity in human HeLa cells measured after 12 hrs by luciferase reporter gene assay, IC50 = 1.2 μM.	27847273
HeLa	Function assay		12 hrs	Inhibition of HIF-1 (unknown origin) expressed in human HeLa cells after 12 hrs by HRE luciferase reporter gene assay, IC50 = 2 μM.	ChEMBL
U251HRE	Function assay			Inhibition of hypoxia-induced HIF1 activation in human U251HRE cells by cell based reporter gene assay, IC50 = 14.8 μM.	18501601
Hep3B	Function assay			Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay, IC50 = 13.8 μM.	17884495
AGS	Function assay			Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay, IC50 = 2 μM.	17884495
Hep3B	Function assay			Inhibition of hypoxia induced HIF1 transcriptional activity in human Hep3B cells by cell-based HRE reporter assay, IC50 = 13.8 μM.	17328532
AGS	Function assay			Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay, IC50 = 2 μM.	17328532
HL60	Cytotoxicity assay			Cytotoxicity against HL60 cells by Propidium iodide exclusion assay, ED50 = 25.27 μM.	17189698
Sf21	Function assay			Activation of sGC Enzyme (soluble Guanylate Cyclase) in Sf21 cells infected with baculo virus in the presence of 30 nM of PAPA/NO, EC50 = 4.11 μM.	11141091
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RXF631L	Growth inhibition assay			Growth inhibition of human RXF631L cells by SRB assay, GI50 = 0.15849 μM.	ChEMBL
NCI-H226	Growth inhibition assay			Growth inhibition of human NCI-H226 cells by SRB assay, GI50 = 0.22387 μM.	ChEMBL
RXF631L	Growth inhibition assay			Growth inhibition of human RXF631L cells by SRB assay, TGI = 0.52481 μM.	ChEMBL
NCI-H226	Growth inhibition assay			Growth inhibition of human NCI-H226 cells by SRB assay, TGI = 0.66069 μM.	ChEMBL
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生物活性

製品説明

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
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].
細胞実験	細胞株	Hep3B cells
	濃度	0.01-10 μM
	反応時間	24 h
	実験の流れ	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.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	HO-1 / HO-2 HIF-1α p-ERK / p-p38 MAPK / p-JNK1 / p-AKT EZH2 / EZH1 / H3K27me3 / Histone H3 DNMT1 / DNMT3a / DNMT3b		18923065
	Growth inhibition assay	Cell proliferation Cell viability		22507221

In Vivo
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].
動物実験	動物モデル	Male nude (BALB/cAnNCrj–nu/nu) mice
	投与量	30 µg/g
	投与経路	i.p.

参考
[1] Martin E, et al. Proc Natl Acad Sci U S A. 2001, 98(23):12938-42. [2] Yeo EJ, et al. J Natl Cancer Inst. 2003, 95(7):516-25.

参考

化学情報

分子量	304.34	化学式	C₁₉H₁₆N₂O₂
CAS No.	170632-47-0	SDF	Download Lificiguat (YC-1) SDFをダウンロードする
Smiles	C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=N2)C4=CC=C(O4)CO
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 61 mg/mL ( (200.43 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 31 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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