Pirmitegravir, also known as STP0404, is a potent and first-in-class ALLINI antiviral agent that targets LEDGF/p75 binding site. STP0404 displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. STP0404 binds to the host LEDGF/p75 protein binding pocket of the IN dimer, which induces aberrant IN oligomerization and blocks the IN-RNA interaction. Consequently, STP0404 inhibits proper localization of HIV-1 RNA genomes in viral particles during viral maturation. Y99H and A128T mutations at the LEDGF/p75 binding pocket render resistance to STP0404. Extensive in vivo pharmacological and toxicity investigations demonstrate that STP0404 harbors outstanding therapeutic and safety properties.
MedKoo Cat#: 465953
Name: Pirmitegravir
CAS#: 2245231-10-9
Chemical Formula: C27H31ClN4O3
Exact Mass: 494.2085
Molecular Weight: 495.02
Elemental Analysis: C, 65.51; H, 6.31; Cl, 7.16; N, 11.32; O, 9.70
The following data is based on the product molecular weight 495.02 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
