YC 1
(Synonyms: 利非西呱,YC-1) 目录号 : GC16406
Lificiguat (YC-1) is a no-dependent soluble guanylyl cyclase(sGC) activator and a Hypoxia-inducible faction-1alpha (HIF-1alpha) inhibitor[1-3].
Cas No.:170632-47-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Hep3B cells |
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Preparation Method |
Cells were placed on a plate and then treated with YC-1 or DMSO for 5 minutes to determine VEGF levels in Normoxia or hypoxia. |
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Reaction Conditions |
0.01-10µM YC-1；24h |
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Applications |
The level of VEGF protein in YC-1 cell culture medium decreased in a dose-dependent manner compared with untreated cells grown under hypoxic conditions. |
| Animal experiment [2]: | |
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Animal models |
Male nude (BALB/cAnNCrj-nu/nu) mice |
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Preparation Method |
Mice(bearing carcinoma) received daily intraperitoneal injections of vehicle or YC-1 (30 microg/g) for 2 weeks. |
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Dosage form |
30 µg/g YC-1; i.p;2 weeks |
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Applications |
YC-1-treated mice tumors expressed lower levels of HIF-1α, less vascularization, and lower levels of HIF-1-inducing genes than control. |
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References: [1]. Yeo EJ, Chun YS, et,al. YC-1: a potential anticancer drug targeting hypoxia-inducible factor 1. J Natl Cancer Inst. 2003 Apr 2;95(7):516-25. doi: 10.1093/jnci/95.7.516. PMID: 12671019. |
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Lificiguat (YC-1) is a no-dependent soluble guanylyl cyclase(sGC) activator and a Hypoxia-inducible faction-1alpha (HIF-1alpha) inhibitor[1-3].
YC-1(0.01-100 µM;24/48 h) inhibits Wnt signaling and suppresses cell proliferation in hepatocellular carcinoma (HCC) [4]. Combination of sorafenib and YC-1(10 µmol/L; 48 h) synergistically inhibited proliferation and colony formation of HepG2, BEL-7402 and HCCLM3 cells[5]. The level of VEGF protein in YC-1 cell culture medium decreased in a dose-dependent manner compared with the VEGF protein level in medium from untreated cells grown under hypoxic conditions[6].
YC-1-treated(30 µg/g;i.p;2 weeks) mice tumors expressed lower levels of HIF-1α, less vascularization, and lower levels of HIF-1-inducing genes than control[6]. 10 mg/kg YC-1(i.p; every three days from day 7 after transplantation) significantly suppressed the growth of both 4T1 and MDA-MB-231 umors[7]. Sevoflurane postconditioning can provide neuroprotection after hypoxic-ischemic injury. Injection of 1.52 µg of the hypoxia-inducible factor-1α inhibitor YC-1 into the left lateral ventricle 30 minutes before hypoxic-ischemic injury reversed the neuroprotection induced by sevoflurane in mice[8].
Lificiguat (YC-1)是一种非依赖性的可溶性鸟酰环化酶(sGC)激活剂,同时他也是缺氧诱导因子-1 α (HIF -1 α)抑制剂[1-3]。
YC-1(0.01-100µM;24/48 h)在肝细胞癌(HCC)中抑制Wnt信号传导并抑制细胞增殖[4]。索拉非尼与YC-1联合用药(10 µM;48 h)协同抑制HepG2、BEL-7402和HCCLM3细胞的增殖和集落形成[5]。与缺氧条件下未经处理的细胞培养液中VEGF蛋白水平相比,YC-1(0.01-10µM；24h)细胞培养液中VEGF蛋白水平呈剂量依赖性下降[6]。
YC-1处理(30µg/g;i.p;2week)小鼠肿瘤表达较低水平的HIF-1α,并且具有较少的血管化以及较低水平的hif -1诱导基因表达[6]。10 mg/kg YC-1(i.p; every three days from day 7 after transplantation)显著抑制了4T1和MDA-MB-231两种肿瘤的生长[7]。七氟醚后处理对缺氧缺血性损伤后的神经系统有保护作用。缺氧缺血性损伤前30分钟向小鼠左侧脑室注射1.52 µg YC-1可逆转七氟醚诱导的神经保护作用[8]。
References:
[1]. 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. doi: 10.1073/pnas.231486198. Epub 2001 Oct 30. PMID: 11687640; PMCID: PMC60803.
[2]. Purohit R, Fritz BG, et,al. YC-1 binding to the β subunit of soluble guanylyl cyclase overcomes allosteric inhibition by the α subunit. Biochemistry. 2014 Jan 14;53(1):101-14. doi: 10.1021/bi4015133. Epub 2013 Dec 30. PMID: 24328155; PMCID: PMC3914721.
[3]. Nayak BK, Shanmugasundaram K, et,al. HIF-1 Mediates Renal Fibrosis in OVE26 Type 1 Diabetic Mice. Diabetes. 2016 May;65(5):1387-97. doi: 10.2337/db15-0519. Epub 2016 Feb 23. PMID: 26908870; PMCID: PMC4839204.
[4]. Wu JY, Shih YL, et,al. YC-1 Antagonizes Wnt/β-Catenin Signaling Through the EBP1 p42 Isoform in Hepatocellular Carcinoma. Cancers (Basel). 2019 May 13;11(5):661. doi: 10.3390/cancers11050661. PMID: 31086087; PMCID: PMC6562864.
[5]. Kong J, Kong F, et,al. YC-1 enhances the anti-tumor activity of sorafenib through inhibition of signal transducer and activator of transcription 3 (STAT3) in hepatocellular carcinoma. Mol Cancer. 2014 Jan 13;13:7. doi: 10.1186/1476-4598-13-7. PMID: 24418169; PMCID: PMC3895679.
[6]. Yeo EJ, Chun YS, et,al. YC-1: a potential anticancer drug targeting hypoxia-inducible factor 1. J Natl Cancer Inst. 2003 Apr 2;95(7):516-25. doi: 10.1093/jnci/95.7.516. PMID: 12671019.
[7]. Li Y, Zhang MZ, et,al. HIF-1α inhibitor YC-1 suppresses triple-negative breast cancer growth and angiogenesis by targeting PlGF/VEGFR1-induced macrophage polarization. Biomed Pharmacother. 2023 May;161:114423. doi: 10.1016/j.biopha.2023.114423. Epub 2023 Feb 21. PMID: 36822023.
[8]. Gao QS, Zhang YH, et,al. Brief inhalation of sevoflurane can reduce glial scar formation after hypoxic-ischemic brain injury in neonatal rats. Neural Regen Res. 2021 Jun;16(6):1052-1061. doi: 10.4103/1673-5374.300456. PMID: 33269750; PMCID: PMC8224129.
| Cas No. | 170632-47-0 | SDF | |
| 别名 | 利非西呱,YC-1 | ||
| 化学名 | (5-(1-benzyl-1H-indazol-3-yl)furan-2-yl)methanol | ||
| Canonical SMILES | OCC1=CC=C(C2=NN(CC3=CC=CC=C3)C4=CC=CC=C42)O1 | ||
| 分子式 | C19H16N2O2 | 分子量 | 304.34 |
| 溶解度 | ≥ 30.4mg/mL in DMSO | 储存条件 | Store at RT |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2858 mL | 16.429 mL | 32.858 mL |
| 5 mM | 0.6572 mL | 3.2858 mL | 6.5716 mL |
| 10 mM | 0.3286 mL | 1.6429 mL | 3.2858 mL |
| 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 | 只 |
| 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。