Lificiguat

• CAT Number: I002226
• CAS Number: 170632-47-0
• Molecular Formula: C19H16N2O2
• Molecular Weight: 304.349
• Purity: ≥95%
• Target: Guanylyl Cyclase
• Solubility: DMSO: ≥ 51 mg/mL
• Storage: Store at RT
• IC50: 0.6-1.1 μM(Kd, in the presence of CO) [1]
• IUPAC Name: [5-(1-benzylindazol-3-yl)furan-2-yl]methanol
• InChI: InChI=1S/C19H16N2O2/c22-13-15-10-11-18(23-15)19-16-8-4-5-9-17(16)21(20-19)12-14-6-2-1-3-7-14/h1-11,22H,12-13H2
• InChIKey: OQQVFCKUDYMWGV-UHFFFAOYSA-N
• SMILES: C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=N2)C4=CC=C(O4)CO

Lificiguat (CAT: I002226) is a potent and selective soluble guanylate cyclase (sGC) stimulator. It works by enhancing the activity of sGC, an enzyme involved in the production of cyclic guanosine monophosphate (cGMP) in cells. By increasing cGMP levels, lificiguat promotes vasodilation and reduces vascular resistance, leading to improved blood flow. This pharmacological activity makes lificiguat a potential therapeutic option for the treatment of pulmonary hypertension, a condition characterized by high blood pressure in the arteries of the lungs. Lificiguat has undergone clinical trials for this indication and has shown promising results in improving exercise capacity and hemodynamic parameters in patients with pulmonary hypertension.

Reference

[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.
[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.
[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.
[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.