DPC-681 is a potent and selective inhibitor ofHIV proteasewith IC90s for wild-typeHIV-1of 4 to 40 nM. IC50 value: 4 - 40 nM [1] Target:HIV proteasein vitro: DPC 681 is extremely potent inhibitor of wild-typeHIV-1. When all of theHIV-1strains 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]

669.85

Solid

C₃₅H₄₈FN₅O₅S

284661-68-3

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL(149.29 mM;Need ultrasonic)

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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。