DPC-681 is a potent and selective inhibitor of HIV protease with IC90s for wild-type HIV-1 of 4 to 40 nM.IC50 value: 4 - 40 nM Target: HIV protease in vitro: DPC 681 is extremely potent inhibitor of wild-type HIV-1. When all of the HIV-1 strains tested are considered, the average concentrations required for 90% inhibition of replication were 7.3 ± 3.4 for DPC 681. DPC 681 shows no loss in potency toward recombinant mutant HIVs with the D30N mutation and a fivefold or smaller loss in potency toward mutant variants with three to five amino acid substitutions.in vivo: The total body clearance (CL) of DPC 681 in dogs was high (1.8 liter/h/kg) equaling hepatic blood flow for this species (1.8 liter/h/kg). After an oral dosing, the Cmax increased ninefold between the 10- and 30-mg/kg DPC 681 dose groups. Bioavailability also increased between the 10- and 30-mg/kg dose groups (18.3 and 78.1%, respectively). These data suggest that hepatic extraction (first-pass effect) can be saturated in the dog. Form:Solid IC50& Target:HIV-1
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DPC-681
CAS number：284661-68-3 molecular formula：C35H48FN5O5S
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| Chinese alias | - | ||
| English alias | DPH 153893 | N-((3-Fluorophenyl)methyl)glycyl-N-((1S,2R)-3-(((3-aminophenyl)sulfonyl)(2-methylpropyl)amino)-2-hydroxy-1-(phenylmethyl)propyl)-3-methyl-L-valinamide | 2-Amino-N-(N-{4-[(3-aminobenzene-1-sulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbuta | ||
| CAS number | 284661-68-3 | molecular formula | C35H48FN5O5S |
| molecular weight | 669.85 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
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