Lopinavir-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 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. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM.
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- CAS No.: 1432060-78-0
- Formule: C37H41D7N4O5
- Masse moléculaire:635.84
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
HIV-1 protease is an essential enzyme for production of mature, infective virus[2].
Lopinavir potently inhibits wild-type and mutant HIV protease (Ki= 1.3 to 3.6 pM), blocks the replication 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)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 1432060-78-0
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Unlabeled CAS 192725-17-0
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Masse moléculaire 635.84
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Formule C37H41D7N4O5
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SMILES
CC1=C(OCC(N[C@@H](CC2=CC=CC=C2)[C@@H](O)C[C@H](CC3=CC=CC=C3)NC([C@H](C([2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])N4C(NCCC4)=O)=O)=O)C(C)=CC=C1
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Synonyms
ABT-378-d7
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Lopinavir-d7 Related Classifications
HY-14588S2 Related Classifications
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