Nelfinavir-d₄ 

Nelfinavir-d₄ is deuterated labeled Nelfinavir (HY-15287). Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (K_i=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent^[1][2][3].

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].
Nelfinavir (AG1341) (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells^[5].
Nelfinavir inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells^[5].
Nelfinavir (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines^[5].
Nelfinavir (5 μM; 0-24 hours) decreases the phosphorylation of AKT^[5].
Nelfinavir activates the cleavage of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, and activates the pro-apoptotic pathway of the unfolded protein response system^[5].
Nelfinavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 35.93 μM^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Nelfinavir (AG1341) (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

571.81

C₃₂H₄₁D₄N₃O₄S

CC(C)(C)NC([C@H]1N(C[C@]2([H])[C@](CCCC2)([H])C1)C[C@](O)([2H])[C@H](CSC3=CC=CC=C3)NC(C4=C(C(O)=CC=C4)C([2H])([2H])[2H])=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]. Bono C, et al. The human immunodeficiency virus-1 protease inhibitor nelfinavir impairs proteasome activity and inhibits the proliferation of multiple myeloma cells in vitro and in vivo. Haematologica. 2012;97(7):1101‐1109.  [Content Brief]

  [3]. Mondal D, et al. Nelfinavir suppresses signaling and nitric oxide production by human aortic endothelial cells: protective effects of thiazolidinediones. Ochsner J. 2013 Spring;13(1):76-90.  [Content Brief]

  [4]. 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]

  [5]. Gills JJ, et al. Nelfinavir, A lead HIV protease inhibitor, is a broad-spectrum, anticancer agent that inducesendoplasmic reticulum stress, autophagy, and apoptosis in vitro and in vivo. Clin Cancer Res. 2007 Sep 1;13(17):5183-94.  [Content Brief]

  [6]. Kaldor SW, et al. Nelfinavir mesylate (AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. J Med Chem. 1997 Nov 21;40(24):3979-85.  [Content Brief]