YC 1|170632-47-0|(利非西呱; YC-1)-陌孚医药/Medlife

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YC 1 (Synonyms: 利非西呱; YC-1)

目录号: PC15256 纯度: ≥98%

CAS No. :170632-47-0

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PC15256-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥750.68	请登录

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中文名称

YC 1

中文别名

3-(5''-羟基甲基-2''-呋喃基)-1-苯基吲哚;3-(5-羟基甲基-2-呋喃基)-1-苯基吲哚;利非西呱;六氢化苯二甲酸;利非西呱,YC-1;3-(5-Hydroxymethyl-2-Furyl)-1-Benzylindazole

英文名称

YC 1

英文别名

1-benzyl-3-(5-hydroxymethyl-furan-2-yl)indazole;2-Furanmethanol,5-[1-(phenylmethyl)-1H-indazol-3-yl]-;lificiguat;YC 1;YC-1;1-Benzyl-3-(5-hydroxymethyl-2-furyl)-1H-indazole;1-benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole;2-Furanmethanol,5-[1-(phenylmethyl)-1H-indazol-3-yl];3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole;5-[1-(PHENYLMETHYL)-1H-INDAZOL-3-YL]-2-FURANMETHANOL;3-(5′-Hydroxymethyl-2′-furyl)-1-benzyl indazole;1-Benzyl-3-(5-hydroxymethylfur-2-yl)indazole;YC 1 (pharmaceutical);Nsc728165;Lificiguat(YC-1);(5-(1-Benzyl-1H-indazol-3-yl)furan-2-yl)Methanol;3-(5-Hydroxymethyl-2-Furyl)-1-Benzylindazole;[5-(1-benzyl-1h-indazol-3-yl)-2-furyl]methanol;515CC1WPTE;OQQVFCKUDYMWGV-UHFFFAOYSA-N;C19H16N2O2;3-(5'-Hydroxymethyl-2'-furyl)-1-benzyl indazole;1-Benzyl-3-(5-hydroxymethyl-2-furyl)indazole;[5-(1-benzylindazol-3-yl)furan-2-yl]methanol;[5-(1-benzyl-1H-indazol-3-yl)furan-2-yl]methanol;5-[1-(Phenylmethyl)-1H-indazo;3-(5/'-hydroxymethyl-2/'-furyl)-1-benzylindazole;YC1;[5-[1-(phenylmethyl)indazo

Cas No.

170632-47-0

分子式

C₁₉H₁₆N₂O₂

分子量

304.34

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with K_d of 0.6-1.1 μM in the presence of CO.

性状

Solid

IC50 & Target[1][2]

Kd: 0.6-1.1 μM (sGC, in the presence of CO)

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 K_d=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 (K_d=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. 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.

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

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. 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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Purohit R, 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. [Information]

[2]. Kong J, 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. [Information]

[3]. Chang LC, et al. YC-1 inhibits proliferation of breast cancer cells by down-regulating EZH2 expression via activation of c-Cbl and ERK. Br J Pharmacol. 2014 Sep;171(17):4010-25. [Information]

[4]. Komsuoglu Celikyurt I, et al. Effects of YC-1 on Learning and Memory Functions of Aged Rats. Med Sci Monit Basic Res. 2014 Aug 21;20:130-7. [Information]

溶解度数据

体外研究:

DMSO : ≥ 100 mg/mL (328.58 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

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
10 mM	0.3286 mL	1.6429 mL	3.2858 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.21 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (8.21 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (8.21 mM) 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.21 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
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玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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