PF-429242 (hydrochloride)

PF-429242 is an inhibitor of site-1 protease with an IC50 value of 170 nM for human recombinant site-1 protease. It is selective for site-1 protease over trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, and furin at concentrations up to 100 µM. PF-429242 completely inhibits proteolytic processing and nuclear translocation of sterol regulatory element-binding protein (SREBP) in HepG2 cells at a concentration of 10 µM. It also reduces expression of HMG-CoA synthase and fatty acid synthase (EC50s = 0.3 and 2 µM, respectively) and inhibits cholesterol synthesis (EC50 = 600 nM) in HepG2 cells and reduces cholesterol and fatty acid synthesis in CD-1 mice. PF-429242 inhibits replication of dengue virus serotypes 1-4 in infected HeLa cells. It also reduces growth of T98G, U87-MG, and A172 glioblastoma cells (IC50s = 0.32, 15.2, and 27.6 µM, respectively).Formal Name: 4-[(diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinyl-benzamide, dihydrochloride. CAS Number: 2248666-66-0. Molecular Formula: C25H35N3O2 . 2HCl. Formula Weight: 482.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 272 nm. SMILES: O=C(C1=CC=C(CN(CC)CC)C=C1)N(CCC2=CC=CC=C2OC)[C@H]3CNCC3.Cl.Cl. InChi Code: 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. InChi Key: GSUZWFZKTIOWTI-MQWQBNKOSA-N.