产品说明书

Lificiguat

Print
Chemical Structure| 170632-47-0 同义名 : YC-1
CAS号 : 170632-47-0
货号 : A174113
分子式 : C19H16N2O2
纯度 : 99%+
分子量 : 304.342
MDL号 : MFCD06407798
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(345.01 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • HIF
描述 YC-1 is an allosteric activator of soluble guanylyl cyclase (sGC). YC-1 exerts antiplatelet effects through the sGC/cyclic GMP pathway[4]. It increased the catalytic rate of the enzyme and sensitizes the enzyme toward its gaseous activators nitric oxide or carbon monoxide. YC-1 activation of sGC can occur independently of heme, but that activation is substantially increased when the heme moiety is present in the enzyme. Administration of YC-1 to experimental animals resulted in the inhibition of the platelet-rich thrombosis and a decrease of the mean arterial pressure, which correlated with increased cGMP levels[5].
作用机制 YC-1 increases the maximal catalytic rate and sensitizes the enzyme toward its gaseous activators by binding to an allosteric site on sGC molecules, thereby reducing the ligand dissociation rate from the heme group.[6]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A498 cells Cytotoxicity assay 48 h Cytotoxicity against human A498 cells incubated for 48 hrs by MTT assay, IC50=0.3 μM 26235951
ACHN cells Function assay 48 h Antitumor activity against human ACHN cells after 48 hrs by MTT assay 20097456
AGS cells Function assay Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay, IC50=2 μM 17328532
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.29mL

0.66mL

0.33mL

16.43mL

3.29mL

1.64mL

32.86mL

6.57mL

3.29mL
参考文献

[1]Wu CC, Ko FN, et al. YC-1 inhibited human platelet aggregation through NO-independent activation of soluble guanylate cyclase. Br J Pharmacol. 1995 Oct;116(3):1973-8.

[2]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. Epub 2001 Oct 30.

[3]Friebe A, Koesling D, et al. Mechanism of YC-1-induced activation of soluble guanylyl cyclase. Mol Pharmacol. 1998 Jan;53(1):123-7.

[4]Wu CC, Ko FN, Kuo SC, Lee FY, Teng CM. YC-1 inhibited human platelet aggregation through NO-independent activation of soluble guanylate cyclase. Br J Pharmacol. 1995 Oct;116(3):1973-8. doi: 10.1111/j.1476-5381.1995.tb16400.x. PMID: 8640334; PMCID: PMC1908948.

[5]Martin E, Lee YC, Murad F. 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.

[6]Friebe A, Koesling D. Mechanism of YC-1-induced activation of soluble guanylyl cyclase. Mol Pharmacol. 1998 Jan;53(1):123-7. doi: 10.1124/mol.53.1.123. PMID: 9443939.