Rupintrivir-d₇  (Synonyms: AG7088-d₇)

Rupintrivir-d7 is a deuterated labeled Rupintrivir^[1]. Rupintrivirvr (AG7088), an antiviral agent, is a potent, selective and irreversible inhibitor of human rhinovirus (HRV) 3C protease. Rupintrivirvr inhibits replication of a panel of 48 different HRV serotypes in H1-HeLA and MRC-5 cell protection assays, with a mean EC₅₀ of 0.023 μM. Rupintrivirvr shows immune-modulatory effect^[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].
In H1-HeLa and MRC-5 cell protection assays, Rupintrivirvr (AG7088) inhibited the replication of all HRV serotypes (48 of 48) tested with a mean 50% effective concentration (EC₅₀) of 0.023 μM (range, 0.003 to 0.081 μM) and a mean EC₉₀ of 0.082 μM (range, 0.018 to 0.261 μM) as well as that of related picornaviruses including coxsackieviruses A21 and B3, enterovirus 70, and echovirus 11^[2].

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

Rupintrivirvr (AG7088) reduces RV-induced TH-2 cytokine IL-4 in precision-cut lung slices (PCLS) of HDM-sensitized mice ex vivo^[3].

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

605.71

C₃₁H₃₂D₇FN₄O₇

223537-30-2

CC1=CC(C(N[C@H](C(C[C@H](C(N[C@H](/C=C/C(OCC)=O)C[C@@H]2CCNC2=O)=O)CC3=CC=C(F)C=C3)=O)C(C([2H])([2H])[2H])(C([2H])([2H])[2H])[2H])=O)=NO1

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]. Patick AK, et al. In vitro antiviral activity of AG7088, a potent inhibitor of human rhinovirus 3C protease. Antimicrob Agents Chemother. 1999 Oct;43(10):2444-50.  [Content Brief]

  [3]. Danov O, et al. Rupintrivir reduces RV-induced TH-2 cytokine IL-4 in precision-cut lung slices (PCLS) of HDM-sensitized mice ex vivo. Respir Res. 2019 Oct 22;20(1):228.  [Content Brief]

  [4]. Dragovich PS, et al. Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 3. Structure-activity studies of ketomethylene-containing peptidomimetics. J Med Chem. 1999 Apr 8;42(7):1203-12.  [Content Brief]