Lificiguat | YC-1 | sGC Activator | AmBeed-信号通路专用抑制剂

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利非西呱 /Lificiguat {[allProObj[0].p_purity_real_show]}

货号：A174113 同义名： YC-1

Lificiguat结合可溶性鸟苷酸环化酶（sGC）的β亚基，在CO存在下Kd为0.6-1.1 μM。

Lificiguat 化学结构
CAS号：170632-47-0

Lificiguat 3D分子结构
CAS号：170632-47-0

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Lificiguat 纯度/质量文件产品仅供科研

货号：A174113 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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HIF 亚型比较

产品名称	HIF ↓ ↑	HIF1 ↓ ↑	PHD1 ↓ ↑	PHD2 ↓ ↑	PHD3 ↓ ↑	其他靶点	纯度
KC7F2	+ HIF-1α, IC50: 20 μM	+ HIF-1α, IC50: 20 μM					98%
Lificiguat	✔						99%+
BAY 87-2243	✔						99%+
PX-478·2HCl	✔						98%+
2-Methoxyestradiol	✔						98%
CAY10585	++ HIF, IC50: 4.4 μM					BCRP	97%
DMOG			✔				98%
FG 2216				++ PHD2, IC50: 3.9 μM			99%+
MK-8617			++++ PHD1, IC50: 1 nM	++++ PHD2, IC50: 1 nM	++++ PHD3, IC50: 14 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Lificiguat 生物活性

靶点	HIF
描述	YC-1 is an allosteric activator of soluble guanylyl cyclase (sGC). YC-1 exerts antiplatelet effects through the sGC/cyclic GMP pathway^[4]. It increased the catalytic rate of the enzyme and sensitizes the enzyme toward its gaseous activators nitric oxide or carbon monoxide. YC-1 activation of sGC can occur independently of heme, but that activation is substantially increased when the heme moiety is present in the enzyme. Administration of YC-1 to experimental animals resulted in the inhibition of the platelet-rich thrombosis and a decrease of the mean arterial pressure, which correlated with increased cGMP levels^[5].
作用机制	YC-1 increases the maximal catalytic rate and sensitizes the enzyme toward its gaseous activators by binding to an allosteric site on sGC molecules, thereby reducing the ligand dissociation rate from the heme group.^[6]

Lificiguat 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A498 cells		Cytotoxicity assay	48 h	Cytotoxicity against human A498 cells incubated for 48 hrs by MTT assay, IC50=0.3 μM	26235951
ACHN cells		Function assay	48 h	Antitumor activity against human ACHN cells after 48 hrs by MTT assay	20097456
AGS cells		Function assay		Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay, IC50=2 μM	17328532
HCT116 cells		Cytotoxicity assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=2.2 μM	24900662

Lificiguat 动物研究

Dose	Mice: 30 mg/kg, 60 mg/kg^[4] (i.p.); 6.96 mg/kg^[5] (i.v.) Rat: 1 mg/kg^[6] (i.p.)
Administration	i.p., i.v.

Lificiguat 参考文献

[1]Wu CC, Ko FN, et al. YC-1 inhibited human platelet aggregation through NO-independent activation of soluble guanylate cyclase. Br J Pharmacol. 1995 Oct;116(3):1973-8.

[2]Martin E, Lee YC, et al. 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. Epub 2001 Oct 30.

[3]Friebe A, Koesling D, et al. Mechanism of YC-1-induced activation of soluble guanylyl cyclase. Mol Pharmacol. 1998 Jan;53(1):123-7.

[4]Wu CC, Ko FN, Kuo SC, Lee FY, Teng CM. YC-1 inhibited human platelet aggregation through NO-independent activation of soluble guanylate cyclase. Br J Pharmacol. 1995 Oct;116(3):1973-8. doi: 10.1111/j.1476-5381.1995.tb16400.x. PMID: 8640334; PMCID: PMC1908948.

[5]Martin E, Lee YC, Murad F. 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. doi: 10.1073/pnas.231486198. Epub 2001 Oct 30. PMID: 11687640; PMCID: PMC60803.

[6]Friebe A, Koesling D. Mechanism of YC-1-induced activation of soluble guanylyl cyclase. Mol Pharmacol. 1998 Jan;53(1):123-7. doi: 10.1124/mol.53.1.123. PMID: 9443939.

Lificiguat 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.29mL

0.66mL

0.33mL

16.43mL

3.29mL

1.64mL

32.86mL

6.57mL

3.29mL

Lificiguat 技术信息

CAS号	170632-47-0
分子式	C₁₉H₁₆N₂O₂
分子量	304.342

别名	YC-1
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 105 mg/mL(345.01 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

A498 cells	Cytotoxicity assay	48 h	Cytotoxicity against human A498 cells incubated for 48 hrs by MTT assay, IC50=0.3 μM	26235951
ACHN cells	Function assay	48 h	Antitumor activity against human ACHN cells after 48 hrs by MTT assay	20097456
AGS cells	Function assay		Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay, IC50=2 μM	17328532
HCT116 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=2.2 μM	24900662
HEK293 cells	Function assay	16 h	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
HeLa cells	Function assay		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
Hep3B cells	Function assay		Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay, IC50=13.8 μM	17884495
HepG2 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50=2.2 μM	24900662
HL60 cells	Cytotoxicity assay	48 h	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, IC50=25.27 μM	23831809
HT1080 cells	Function 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, IC50=48.4 μM	25773014
NCI-H226 cells	Function assay	48 h	Antitumor activity against human NCI-H226 cells after 48 hrs by MTT assay, IC50=1.9 μM	20097456
U251HRE cells	Function assay		Inhibition of hypoxia-induced HIF1 activation in human U251HRE cells by cell based reporter gene assay, IC50=14.8 μM	18501601

利非西呱 /Lificiguat {[allProObj[0].p_purity_real_show]}

Lificiguat 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Lificiguat 质控信息

Lificiguat 生物活性

Lificiguat 细胞研究

Lificiguat 动物研究

Lificiguat 参考文献

Lificiguat 实验方案

Lificiguat 技术信息

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利非西呱 /Lificiguat {[allProObj[0].p_purity_real_show]}

Lificiguat 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Lificiguat 质控信息

Lificiguat 生物活性

Lificiguat 细胞研究

Lificiguat 动物研究

Lificiguat 参考文献

Lificiguat 实验方案

Lificiguat 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Lificiguat 纯度/质量文件产品仅供科研