Lificiguat (YC-1)是一種非依賴性的可溶性鳥(niǎo)酰環(huán)化酶(sGC)激活劑,同時(shí)他也是缺氧誘導(dǎo)因子-1 α (HIF -1 α)抑制劑[1-3]。

YC-1(0.01-100μM;24/48 h)在肝細(xì)胞癌(HCC)中抑制Wnt信號(hào)傳導(dǎo)并抑制細(xì)胞增殖[4]。索拉非尼與YC-1聯(lián)合用藥(10 μM;48 h)協(xié)同抑制HepG2、BEL-7402和HCCLM3細(xì)胞的增殖和集落形成[5]。與缺氧條件下未經(jīng)處理的細(xì)胞培養(yǎng)液中VEGF蛋白水平相比,YC-1(0.01-10μM；24h)細(xì)胞培養(yǎng)液中VEGF蛋白水平呈劑量依賴性下降[6]。

YC-1處理(30μg/g;i.p;2week)小鼠腫瘤表達(dá)較低水平的HIF-1α,并且具有較少的血管化以及較低水平的hif -1誘導(dǎo)基因表達(dá)[6]。10 mg/kg YC-1(i.p; every three days from day 7 after transplantation)顯著抑制了4T1和MDA-MB-231兩種腫瘤的生長(zhǎng)[7]。七氟醚后處理對(duì)缺氧缺血性損傷后的神經(jīng)系統(tǒng)有保護(hù)作用。缺氧缺血性損傷前30分鐘向小鼠左側(cè)腦室注射1.52 μg YC-1可逆轉(zhuǎn)七氟醚誘導(dǎo)的神經(jīng)保護(hù)作用[8]。

產(chǎn)品性質(zhì)：

Cas No.:170632-47-0

別名:利非西呱,YC-1

化學(xué)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

儲(chǔ)存條件:Store at RT

注意事項(xiàng)：

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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.