Pirmitegravir (STP0404) | HIV-1 integrase inhibitor

Chemical Structure : STP0404

CAS No.: 2245231-10-9

STP0404 (Pirmitegravir)

Catalog No.: PC-73436Not For Human Use, Lab Use Only.

Pirmitegravir (STP0404) is a highly potent, first-in-class, allosteric HIV-1 integrase inhibitor (ALLINI) with IC50 of 0.41 nM against HIV-1NL4-3 in human PBMCs.

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Biological Activity

Pirmitegravir (STP0404) is a highly potent, first-in-class, allosteric HIV-1 integrase inhibitor (ALLINI) with IC50 of 0.41 nM against HIV-1NL4-3 in human PBMCs.

STP0404 inhibited dual tropic HIV-189.6 at 1.4 nM IC50 in CEMx174 cells.

STP0404 inhibited IN-LEDGF/p75 binding with IC50 of 0.19 uM in HTRF-based assay.

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.

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.

Physicochemical Properties

M.Wt	495.020
Formula	C27H31ClN4O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-2-(tert-butoxy)-2-(4-(4-chlorophenyl)-2,3,6-trimethyl-1-((1-methyl-1H-pyrazol-4-yl)methyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)acetic acid

References

1. Maehigashi T, et al. PLoS Pathog. 2021 Jul 22;17(7):e1009671.

STP0404 (Pirmitegravir)

Biological Activity

Physicochemical Properties

References

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