2. GPCR/G Protein
  3. Guanylate Cyclase
  4. Lificiguat

Lificiguat  (Synonyms: 利非西呱; YC-1)

目录号: HY-14927 纯度: 99.74%
COA 产品使用指南

摩尔计算器

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

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Lificiguat Chemical Structure

Lificiguat Chemical Structure

CAS No. : 170632-47-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥605
In-stock
5 mg ￥550
In-stock
10 mg ￥770
In-stock
50 mg ￥2800
In-stock
100 mg ￥4363
In-stock
200 mg 现货 询价
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Customer Review

Lificiguat 相关抗体

Top Publications Citing Use of Products

    Lificiguat purchased from MCE. Usage Cited in: Radiat Environ Biophys. 2019 Aug;58(3):439-448.  [Abstract]

    Western blot analysis reveals HIF-1α and BCL-2 expression in the four types of H1299 cells exposed to radiation following YC-1 pretreatment. β-actin level is determined as internal control.

    Lificiguat purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Nov;107:1736-1743.  [Abstract]

    Western blot is used to assess the protein levels of VEGF, Ang-2, ALP, Runx2, and OPN-1 in the co-culture of HUVEC-12 and BMSCs. β-actin is used as a loading control.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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]
    体外研究
    (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].

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

    Lificiguat 相关抗体:
    体内研究
    (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.
    分子量

    304.34

    Formula

    C19H16N2O2
    CAS 号
    性状

    固体

    颜色

    Off-white to yellow

    中文名称

    利非西呱
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (328.58 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (8.21 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (8.21 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.74%

    COA (203 KB) LCMS (94 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    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
    [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
    [3][4]

    Mice[3]
    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.
    Rats[4]
    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.
    参考文献

    Lificiguat 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.2858 mL 16.4290 mL 32.8580 mL 82.1450 mL
    5 mM 0.6572 mL 3.2858 mL 6.5716 mL 16.4290 mL
    10 mM 0.3286 mL 1.6429 mL 3.2858 mL 8.2145 mL
    15 mM 0.2191 mL 1.0953 mL 2.1905 mL 5.4763 mL
    20 mM 0.1643 mL 0.8214 mL 1.6429 mL 4.1072 mL
    25 mM 0.1314 mL 0.6572 mL 1.3143 mL 3.2858 mL
    30 mM 0.1095 mL 0.5476 mL 1.0953 mL 2.7382 mL
    40 mM 0.0821 mL 0.4107 mL 0.8214 mL 2.0536 mL
    50 mM 0.0657 mL 0.3286 mL 0.6572 mL 1.6429 mL
    60 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3691 mL
    80 mM 0.0411 mL 0.2054 mL 0.4107 mL 1.0268 mL
    100 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8214 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Lificiguat170632-47-0YC-1利非西呱YC1YC 1Guanylate CyclaseInhibitorinhibitorinhibit

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