| Bioactivity | 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 | HIV-1 protease is an essential enzyme for production of mature, infective virus[1].Lopinavir potently inhibits wild-type and mutant HIV protease (Ki= 1.3 to 3.6 pM), blocks the replication of laboratory and clinical strains of HIV type 1 (EC50=0.006 to 0.017 μM), and maintains high potency against mutant HIV selected by Ritonavir in vivo (EC50=≤0.06 μM)[2]. | ||||||||||||
| In Vivo | Coadministration with low-dose Ritonavir significantly improves the pharmacokinetic properties and hence the activity of Lopinavir against HIV-1 protease[1]. | ||||||||||||
| Name | Lopinavir | ||||||||||||
| CAS | 192725-17-0 | ||||||||||||
| Formula | C37H48N4O5 | ||||||||||||
| Molar Mass | 628.80 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Cvetkovic RS, et al. Lopinavir/ritonavir: a review of its use in the management of HIV infection. Drugs. 2003;63(8):769-802. [2]. Sham HL, et al. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother. 1998;42(12):3218-3224. [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. |
Lopinavir
CAS: 192725-17-0 F: C37H48N4O5 W: 628.80
Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6
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