| Bioactivity | Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis 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 3CLpro inhibitor with an IC50 of 14.2 μM[3]. |
| Invitro | 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 (Ki=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. 0 --> Lopinavir-d7 相关抗体: |
| In Vivo | 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. |
| CAS | 1432060-78-0 |
| Formula | C37H41D7N4O5 |
| Molar Mass | 635.84 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [2]. Cvetkovic RS, et al. Lopinavir/ritonavir: a review of its use in the management of HIV infection. Drugs. 2003;63(8):769-802. [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. [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. |
Lopinavir-d7
CAS: 1432060-78-0 F: C37H41D7N4O5 W: 635.84
Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimeti
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This product is for research use only, not for human use. We do not sell to patients.