| Identification | Back Directory | [Name]
DPC-681 | [CAS]
284661-68-3 | [Synonyms]
DPC-681
DPH-153893
L-Valinamide, N-[(3-fluorophenyl)methyl]glycyl-N-[(1S,2R)-3-[[(3-aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-3-methyl- | [Molecular Formula]
C35H48FN5O5S | [MOL File]
284661-68-3.mol | [Molecular Weight]
669.85 |
| Chemical Properties | Back Directory | [density ]
1.217±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
13.52±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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 [1]
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. [1]
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. [1] | [IC 50]
HIV-1 | [storage]
Store at -20°C | [References]
[1] Kaltenbach RF 3rd, et al. DPC 681 and DPC 684: potent, selective inhibitors of human immunodeficiency virus protease active against clinically relevant mutant variants. Antimicrob Agents Chemother. 2001 Nov;45(11):3021-8. DOI:10.1128/AAC.45.11.3021-3028.2001 |
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Musechem
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DC Chemicals
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