Description | Bevirimat (PA-457) is a first-in-class inhibitor of HIV-1 maturation, blocking the cleavage of the Gag capsid (CA) precursor, CA-SPI, to mature CA protein during virion maturation. |
In vivo | 在一项临床研究中,PA-457通过单次口服给药,在HIV感染的成人中以剂量依赖的方式降低了病毒载量[1]。 |
Synonyms | YK FH312, MPC-4326, PA-457, 贝韦立马 |
molecular weight | 584.83 |
Molecular formula | C36H56O6 |
CAS | 174022-42-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility | DMSO: 50 mg/mL (85.49 mM) |
References | 1. Smith P F , Ogundele A , Forrest A , et al. Phase I and II Study of the Safety, Virologic Effect, and Pharmacokinetics/Pharmacodynamics of Single-Dose 3-O-(3′,3′-Dimethylsuccinyl)Betulinic Acid (Bevirimat) against Human Immunodeficiency Virus Infection[J]. Antimicrobial Agents & Chemotherapy, 2007, 51(10):3574. 2. Purdy MD, Shi D, Chrustowicz J,et al.MicroED structures of HIV-1 Gag CTD-SP1 reveal binding interactions with the maturation inhibitor bevirimat[J].Proc Natl Acad Sci U S A. 2018 Dec 26;115(52):13258-13263. 3. Stoddart C A , Pheroze J , Barbara S , et al. Potent Activity of the HIV-1 Maturation Inhibitor Bevirimat in SCID-hu Thy/Liv Mice[J]. PLoS ONE, 2007, 2(11):e1251-. |