PF429242 dihydrochloride

• CAT Number: I020654
• CAS Number: 2248666-66-0
• Molecular Formula: C₂₅H₃₇Cl₂N₃O₂
• Molecular Weight: 482.49
• Purity: ≥95%
• Storage: Store at -20°C
• IUPAC Name: 4-(diethylaminomethyl)-N-[2-(2-methoxyphenyl)ethyl]-N-[(3R)-pyrrolidin-3-yl]benzamide;dihydrochloride
• InChI: InChI=1S/C25H35N3O2.2ClH/c1-4-27(5-2)19-20-10-12-22(13-11-20)25(29)28(23-14-16-26-18-23)17-15-21-8-6-7-9-24(21)30-3;;/h6-13,23,26H,4-5,14-19H2,1-3H3;2*1H/t23-;;/m1../s1
• InChIKey: GSUZWFZKTIOWTI-MQWQBNKOSA-N
• SMILES: CCN(CC)CC1=CC=C(C=C1)C(=O)N(CCC2=CC=CC=C2OC)C3CCNC3.Cl.Cl

PF429242 dihydrochloride（Cat No.:I020654） is a reversible and competitive inhibitor of SREBP site 1 protease (S1P), with an IC50 value of 175 nM. S1P is a key enzyme in the regulation of cholesterol and fatty acid metabolism. Inhibition of S1P by PF429242 dihydrochloride leads to a reduction in the production of cholesterol and other lipids. This compound has potential applications in the treatment of hyperlipidemia, a condition characterized by abnormally high levels of lipids in the blood, which can increase the risk of heart disease.

Reference

[1]. Hawkins JL, et al. Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J Pharmacol Exp Ther. 2008 Sep;326(3):801-8.[2]. Uchida L, et al. Suppressive Effects of the Site 1 Protease (S1P) Inhibitor, PF-429242, on Dengue Virus Propagation. Viruses. 2016 Feb 10;8(2). pii: E46. doi: 10.3390/v8020046.[3]. Urata S, et al. Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J Virol. 2011 Jan;85(2):795-803.