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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1432060-78-0
- 分子式: C37H41D7N4O5
- 分子量:635.84
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
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.
化学情報
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CAS 番号 1432060-78-0
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非標識Cas 192725-17-0
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分子量 635.84
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分子式 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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別名
ABT-378-d7
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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