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Lificiguat (YC-1)
中文名稱：利非西呱
Lificiguat (YC-1)是一種不依賴于NO的soluble guanylyl cyclase(sGC)激活劑和Hypoxia-inducible factor-1alpha (HIF-1alpha)抑制劑。
Lificiguat (YC-1) Chemical Structure
CAS: 170632-47-0
產(chǎn)品質(zhì)控
批次：
純度：
99.94%
99.94
Lificiguat (YC-1)相關(guān)產(chǎn)品
| 相關(guān)靶點 | HIF1 HIF2 PHD1 PHD2 PHD3 | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | PX-478 2HCl BAY 87-2243 KC7F2 IOX2 CAY10585 (LW 6) Molidustat (BAY 85-3934) PT2385 IDF-11774 MK-8617 Daprodustat (GSK1278863) FG-2216 Vadadustat Glucosamine Enarodustat (JTZ-951) SYP-5 IOX4 | 點擊展開 |
| 相關(guān)化合物庫 | 酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫 血管生成相關(guān)化合物庫 HIF-1信號通路化合物庫 FDA抗癌藥物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Lificiguat (YC-1)是一種不依賴于NO的soluble guanylyl cyclase(sGC)激活劑和Hypoxia-inducible factor-1alpha (HIF-1alpha)抑制劑。 | ||
|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | YC-1是可溶性鳥苷酸環(huán)化酶（sGC）的變構(gòu)激活劑。YC-1能增強該酶的催化速率，并使sGC對一氧化氮氣體活化劑或一氧化碳敏感化。YC-1單獨使用只能激活sGC10倍，但它能增強sGC依賴于CO和NO的激活效力，導(dǎo)致高度純化的酶激活，其效力可達數(shù)百倍到數(shù)千倍[1]。在體外，YC-1能夠抑制血小板聚集、血管收縮和HIF-1活性。YC-1可在轉(zhuǎn)錄后水平上完全抑制HIF-1α的表達，因此在低氧條件下抑制肝癌細胞中的HIF-1的轉(zhuǎn)錄因子活性，這說明YC-1的作用可能與氧傳感通路相關(guān)，而不是sGC相關(guān)[2]。 | |||
|---|---|---|---|---|
| 細胞實驗 | 細胞系 | Hep3B細胞 | ||
| 濃度 | 0.01-10 μM | |||
| 孵育時間 | 24 h | |||
| 方法 | 將Hep3B細胞以1 × 105細胞/孔的密度鋪于6孔板中，加入含10%熱滅活FBS的α-modified Eagle medium，培養(yǎng)過夜。然后用0.01-10 μM YC-1或DMSO處理細胞5分鐘，然后置于常氧或低氧環(huán)境下24小時。測定VEGF水平。 | |||
| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | 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 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 將YC-1作用于實驗動物，導(dǎo)致富含血小板的血栓形成受到抑制、平均動脈血壓降低(與cGMP水平上升相關(guān))[1]。YC-1在負瘤小鼠中能有效地抑制腫瘤生長。YC-1處理過的小鼠腫瘤中HIF-1活性的抑制與血管生成、腫瘤生長受到抑制相關(guān)。而YC-1的抗血小板凝集效果并不影響腫瘤生長[2]。 | |
|---|---|---|
| 動物實驗 | Animal Models | Male nude (BALB/cAnNCrj–nu/nu) mice |
| Dosages | 30 μg/g | |
| Administration | i.p. | |
化學(xué)信息&溶解度
| 分子量 | 304.34 | 分子式 | C19H16N2O2 |
| CAS號 | 170632-47-0 | SDF | Download Lificiguat (YC-1) SDF |
| Smiles | C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=N2)C4=CC=C(O4)CO | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 61 mg/mL ( (200.43 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 31 mg/mL (101.85 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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