Lopinavir-d₇  (Synonyms: 洛匹那韦-d₇; ABT-378-d₇)

Lopinavir-d₇ is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity^[1][2]. Lopinavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 14.2 μM^[3].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
HIV-1 蛋白酶是产生成熟的感染性病毒的必需酶^[2]。
Lopinavir 有效抑制野生型和突变型 HIV 蛋白酶 (K_i=1.3 至 3.6 pM)，阻止 HIV 菌株的复制 (EC₅₀=0.006 至 0.017 μM)，并在体内保持对利托那韦选择的突变 HIV 的高效力 (EC ₅₀=≤0.06 μM)^[3]。

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

与低剂量利托那韦共同给药可显著改善 Lopinavir 的药代动力学特性，从而改善其抗 HIV-1 蛋白酶的活性^[2]。

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

635.84

C₃₇H₄₁D₇N₄O₅

1432060-78-0

洛匹那韦-d₇

Room temperature in continental US; may vary elsewhere.

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

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Cvetkovic RS, et al. Lopinavir/ritonavir: a review of its use in the management of HIV infection. Drugs. 2003;63(8):769-802.  [Content Brief]

  [3]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.  [Content Brief]

  [4]. Sham HL, et al. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother. 1998;42(12):3218-3224.  [Content Brief]