| Description | L 756423 (L756423) is a novel potent and selective and competitive HIV protease inhibitor with a Ki value of 0.049 nM for HIV-1 PR.L 756423 blocks the spread of HIV(IIIb)-infected MT25 lymphocytes at 0.50-0.1 nM and can be used for the study of Acquired Immunodeficiency Syndrome (AIDS). |
| In vitro | MK-944a (L-756,423) is selective and competitively inhibits HIV-1 PR with a K(i) value of 0.049 nM. It stops the spread of the HIV(IIIb)-infected MT4 lymphoid cells at 25.0-50.0 nM, even in the presence of alpha(1) acid glycoprotein, human serum albumin, normal human serum, or fetal bovine serum.[1] |
| Synonyms | L756423, MK-944a, MK944a, L-756,423, L-756423, MK 944a |
| molecular weight | 652.82 |
| Molecular formula | C39H48N4O5 |
| CAS | 216863-66-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (76.59 mM) |
| References | 1. Dorsey BD, et al. Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors. J Med Chem. 2000 Sep 7;43(18):3386-99. 2. Rose MJ, et al. Determination of L-756 423, a novel HIV protease inhibitor, in human plasma and urine using high-performance liquid chromatography with fluorescence detection. J Chromatogr B Biomed Sci Appl. 1999 Sep 24;732(2):425-35. 3. Rose MJ, et al. High-throughput simultaneous determination of the HIV protease inhibitors indinavir and L-756423 in human plasma using semi-automated 96-well solid phase extraction and LC-MS/MS. J Pharm Biomed Anal. 2000 Dec 15;24(2):291-305. 4. Rose MJ, et al. Determination of L-756 423, a novel HIV protease inhibitor, in human plasma and urine using high-performance liquid chromatography with fluorescence detection. J Chromatogr B Biomed Sci Appl. 1999 Sep 24;732(2):425-35. |