DPC 684 

DPC 684 is a potent and selective HIV-1 protease inhibitor (IC₉₀ = 5.7-40 nM, Ki = 0.021 nM). DPC 684 competitively inhibits HIV-1 protease and blocks viral polyprotein cleavage. DPC 684 has low protein binding and broad-spectrum inhibition against a variety of wild-type and mutant HIV-1 proteases. DPC 684 has low protein binding and broad-spectrum inhibition (IC₉₀ = 1.9-6.3 nM). DPC 684 has research significance for HIV^[1].

DPC 684 (Compound DPC 684) 在不同细胞模型中 (MT-2: HIV-1 RF, IIIB毒株, PBMC: HIV-1 IIIB, NL4-3毒株)， 90 % 抑制病毒复制所需的平均浓度为 14.5 nM，具有广谱抗 HIV-1 活性^[1]。

DPC 684 针对实验室和临床分离株的抗病毒活性为 (IC₉₀: RF 为 5.7 nM, 7.8 nM; HXB2 为 12 nM; NL4-3为 20 nM; IIIB 为 8.8 nM, 40 nM; Thai 9466 和 Patient E 为 11 nM; HIV-2 为 32 nM)^[1]。

DPC 684 在 MT-2 细胞中，对临床常见耐药突变保持高效性，D30N 突变时 IC₉₀ = 8.8 ，无效力损失。多重突变时 IC₉₀ = 26 ，2倍损失^[1]。

DPC 684 在浓度为 13 μM 时对肾素、胃蛋白酶等 17 种人蛋白酶均无显著抑制，证明其高选择性抑制 HIV蛋白酶^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

DPC 684 (Compound DPC 684) 在大鼠和犬类中进行的为期 2 周的安全性评估研究中，大鼠肝脏出现组织学变化，犬类出现心电图轻度Ⅰ度房室传导阻滞，在推进研究时需重点关注这些靶器官的潜在风险^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

669.85

C₃₅H₄₈FN₅O₅S

284661-73-0

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. R F Kaltenbach 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.  [Content Brief]