Bioactivity | (rel)-Lopinavir-d8 ((rel)-ABT-378-d8)is the deuterium labeledLopinavir(HY-14588)[1]. 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[2][3]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[4]. |
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]。 |
Name | (rel)-Lopinavir-d8 |
CAS | 1322625-54-6 |
Formula | C37H40D8N4O5 |
Molar Mass | 636.85 |
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. |