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 proteasein 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.

Product information

CAS Number: 284661-68-3

Molecular Weight: 669.85

Formula: C35H48FN5O5S

Chemical Name: (2S)-2-(2-{[(3-fluorophenyl)methyl]amino}acetamido)-N-[(2S,3R)-3-hydroxy-4-[N-(2-methylpropyl)3-aminobenzenesulfonamido]-1-phenylbutan-2-yl]-3,3-dimethylbutanamide

Smiles: CC(C)CN(C[C@@H](O)[C@H](CC1=CC=CC=C1)NC(=O)[C@@H](NC(=O)CNCC1=CC=CC(F)=C1)C(C)(C)C)S(=O)(=O)C1C=CC=C(N)C=1

InChiKey: PNIFFZXGBAYVMQ-RKKDRKJOSA-N

InChi: InChI=1S/C35H48FN5O5S/c1-24(2)22-41(47(45,46)29-16-10-15-28(37)19-29)23-31(42)30(18-25-11-7-6-8-12-25)39-34(44)33(35(3,4)5)40-32(43)21-38-20-26-13-9-14-27(36)17-26/h6-17,19,24,30-31,33,38,42H,18,20-23,37H2,1-5H3,(H,39,44)(H,40,43)/t30-,31+,33+/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.