Lificiguat (YC-1)

For research use only. Not for use in humans.

目录号:S7958 中文名称:利非西呱

Lificiguat (YC-1) Chemical Structure

CAS No. 170632-47-0

Lificiguat (YC-1)是一种不依赖于NO的soluble guanylyl cyclase(sGC)激活剂和Hypoxia-inducible factor-1alpha (HIF-1alpha)抑制剂。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 794.43 现货
RMB 794.88 现货
RMB 3251.51 现货
RMB 8166.33 现货
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客户使用Selleck生产的Lificiguat (YC-1)发表文献15篇:

产品安全说明书

HIF抑制剂选择性比较

生物活性

产品描述 Lificiguat (YC-1)是一种不依赖于NO的soluble guanylyl cyclase(sGC)激活剂和Hypoxia-inducible factor-1alpha (HIF-1alpha)抑制剂。
靶点
sGC [1] HIF-1α [2]
体外研究

YC-1是可溶性鸟苷酸环化酶(sGC)的变构激活剂。YC-1能增强该酶的催化速率,并使sGC对一氧化氮气体活化剂或一氧化碳敏感化。YC-1单独使用只能激活sGC10倍,但它能增强sGC依赖于CO和NO的激活效力,导致高度纯化的酶激活,其效力可达数百倍到数千倍[1]。在体外,YC-1能够抑制血小板聚集、血管收缩和HIF-1活性。YC-1可在转录后水平上完全抑制HIF-1α的表达,因此在低氧条件下抑制肝癌细胞中的HIF-1的转录因子活性,这说明YC-1的作用可能与氧传感通路相关,而不是sGC相关[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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NCI-H226 NWOzVZNRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkPIS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUmNKNUh{Mk[gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyIE2gNE4zOjN6NzFOwG0v M4fZW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM{Ozl6NT:nQmNpTU2ETEyvZV4>
RXF631L M4j5UGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2jG[Gdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJHJZTjZ|MVygZ4VtdHNiYomgV3JDKGG|c3H5MEBVT0liPTCwMlUzPDhzIN88UU4> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzN|M6QDVxJ{7DbGVOSkx:L3G+
NCI-H226 M1X3[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHr5RmdIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKyOkBk\WyuczDifUBUWkJiYYPzZZktKFSJSTC9JFAvPjZyNkmg{txONg>? NILUe4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OzN7OEWvK|5EcEWPQly8M4E,
HeLa NXvWdnBITnWwY4Tpc44h[XO|YYm= M1K4[VEzKGi{cx?= NWqwNVBkUW6qaXLpeIlwdiCxZjDITWYuOSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDoeY1idiCKZVzhJINmdGy|IHHmeIVzKDF{IHjyd{BjgSCKUlWgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwJF0hOiEQvF2u NHLxNIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OzN7OEWvK|5EcEWPQly8M4E,

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
HO-1 / HO-2 ; 

PubMed: 18923065     


Concentration-dependent effect of YC-1 (5-100 μM for 24 h) on HO-1 and HO-2 protein expression. 

HIF-1α; 

PubMed: 22507221     


Under normoxic conditions, 10 µmol/L YC-1 has no effect on HIF-1α protein (B). Under hypoxic conditions, YC-1 inhibited protein expression (D) in a dose-dependent manner.

p-ERK / p-p38 MAPK / p-JNK1 / p-AKT ; 

PubMed: 18923065     


Effect of YC-1 (50 μM for 0-30 min) treatment on ERK1/2, p38 MAPK, JNK, and Akt activity. 

EZH2 / EZH1 / H3K27me3 / Histone H3 ; 

PubMed: 24697523     


Cells were treated with the indicated concentrations of YC-1 (MDA-MB-468: 24 h; SKBR3: 30 h; A) or 3 μM YC-1 for the indicated times 

DNMT1 / DNMT3a / DNMT3b ; 

PubMed: 24697523     


MDA-MB-468 and SKBR3 cells were treated with the indicated concentrations of YC-1 for 24 h (MDA-MB-468) or 30 h (SKBR3). Cell lysates were prepared and analysed by Western blotting.

18923065 22507221 24697523
Growth inhibition assay
Cell proliferation; 

PubMed: 22507221     


A, YC-1 inhibits MDA-MB-468 cell proliferation significantly under normoxia. B, YC-1 (3 and 10 µmol/L) inhibits MDA-MB-468 cell proliferation significantly under hypoxia. *P < 0.001, vs. control.

Cell viability; 

PubMed: 22507221     


Various breast cancer cell lines were treated with the indicated concentrations of YC-1 for 72 h. Cell viability was determined by the MTT method.

22507221
体内研究 将YC-1作用于实验动物,导致富含血小板的血栓形成受到抑制、平均动脉血压降低(与cGMP水平上升相关)[1]。YC-1在负瘤小鼠中能有效地抑制肿瘤生长。YC-1处理过的小鼠肿瘤中HIF-1活性的抑制与血管生成、肿瘤生长受到抑制相关。而YC-1的抗血小板凝集效果并不影响肿瘤生长[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[2]
- 合并
  • Cell lines: Hep3B细胞
  • Concentrations: 0.01-10 μM
  • Incubation Time: 24 h
  • Method: 将Hep3B细胞以1 × 105细胞/孔的密度铺于6孔板中,加入含10%热灭活FBS的α-modified Eagle medium,培养过夜。然后用0.01-10 μM YC-1或DMSO处理细胞5分钟,然后置于常氧或低氧环境下24小时。测定VEGF水平。
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: Male nude (BALB/cAnNCrj–nu/nu) mice
  • Dosages: 30 µg/g
  • Administration: i.p.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 60 mg/mL (197.14 mM)
Water Insoluble
Ethanol '60 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 304.34
化学式

C19H16N2O2

CAS号 170632-47-0
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID