GLPBio

Rupintrivir

Catalog No.: GC50441Purity:>98.00%Synonyms: AG7088
COASDSData Sheet
Rupintrivirvr (AG7088), ein antivirales Medikament, ist ein potenter, selektiver und irreversibler Inhibitor der 3C-Protease des humanen Rhinovirus (HRV).

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Rupintrivir
Cas No.: 223537-30-2
10mM (in 1mL DMSO)In Stock
$246.00
1
1mgIn Stock
$82.00
1
5mgIn Stock
$186.00
1
10mgIn Stock
$311.00
1
25mgIn Stock
$494.00
1
50mgIn Stock
$673.00
1
100mgIn Stock
$888.00
1
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Zitate (Citations)

1 publicationsPublikationen von Forschern, die dieses Produkt verwenden

Beschreibung (Description)

Rupintrivir is a potent, irreversible inhibitor of human rhinovirus (HRV) 3C protease with a mean EC50 value of 0.023μM for inhibiting the replication of all HRV serotypes [1]. Rupintrivir binds in a unique conformation to the active site of SARS-CoV-2 Mpro, splitting the catalytic cysteine and histidine residues and inhibiting the activity of SARS-CoV-2 [2]. Rupintrivir has been widely used to inhibit the replication of enterovirus 71 (EV 71), and is combined with IFN-α to develop combination therapies that efficiently eliminate the virus [3].

In vitro, Rupintrivir treatment for 72 hours significantly reduced the levels of Norovirus RNA in HG23 cells, with an EC50 value of 0.3µM[4]. Treatment with 100nM Rupintrivir for 48 hours suppressed the HRV-induced hypersecretion of cytokines IL-6 and IL-4 in precision-cut lung slices (PCLS) from house dust mite (HDM)-sensitized mice [5].

In vivo, Rupintrivir treatment via daily intraperitoneal injection at a dose of 0.1mg/kg for 10 days can alleviate EV 71 virus-induced necrotizing myositis in suckling mice and increase the survival rate[6].

References:
[1] Patick A K, Binford S L, Brothers M A, et al. In vitro antiviral activity of AG7088, a potent inhibitor of human rhinovirus 3C protease[J]. Antimicrobial agents and chemotherapy, 1999, 43(10): 2444-2450.
[2] Lockbaum G J, Henes M, Lee J M, et al. Pan-3C protease inhibitor rupintrivir binds SARS-CoV-2 main protease in a unique binding mode[J]. Biochemistry, 2021, 60(39): 2925-2931.
[3] Hung H C, Wang H C, Shih S R, et al. Synergistic inhibition of enterovirus 71 replication by interferon and rupintrivir[J]. Journal of Infectious Diseases, 2011, 203(12): 1784-1790.
[4] Rocha-Pereira J, Nascimento M S J, Ma Q, et al. The enterovirus protease inhibitor rupintrivir exerts cross-genotypic anti-norovirus activity and clears cells from the norovirus replicon[J]. Antimicrobial agents and chemotherapy, 2014, 58(8): 4675-4681.
[5] Danov O, Lasswitz L, Obernolte H, et al. Rupintrivir reduces RV-induced TH-2 cytokine IL-4 in precision-cut lung slices (PCLS) of HDM-sensitized mice ex vivo[J]. Respiratory research, 2019, 20(1): 228.
[6] Zhang X, Song Z, Qin B, et al. Rupintrivir is a promising candidate for treating severe cases of enterovirus-71 infection: evaluation of antiviral efficacy in a murine infection model[J]. Antiviral research, 2013, 97(3): 264-269.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

HG23 cells

Preparation Method

HG23 cells (Norwalk virus replicon-bearing Huh-7 origin) were grown in RPMI-1640 medium with 10% (v/v) fetal bovine serum (FBS), 2mM l-glutamine, 20mM HEPES, 0.075g/l sodium bicarbonate, 100U penicillin/ml, and 100μg/ml streptomycin at 37°C and 1.25mg/ml of Geneticin (G418) in a humidified atmosphere of 5% CO2. Cells were seeded in 96-well plates at a density of 5×103 cells and cultured overnight. A serial dilution of Rupintrivir (0.1, 0.2, 0.4, 0.8, 1.6, 3.1, and 6.3µM) was added to the cultures. After 72h of incubation, cell monolayers were washed with phosphate-buffered saline (PBS) and collected for quantification of RNA load by qRT-PCR.

Reaction Conditions

0.1, 0.2, 0.4, 0.8, 1.6, 3.1, and 6.3µM; 72h

Applications

Rupintrivir treatment significantly reduced the levels of Norovirus RNA in HG23 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

Suckling ICR mice

Preparation Method

Two-day-old suckling ICR mice (2.0-2.3g) were injected with 106 pfu EV71 (strain 695F) and subsequently underwent intraperitoneal (i.p.) injection with 5-15μl of Rupintrivir or ribavirin dissolved in DMSO to achieve a dosage of 0.1mg/kg (n=13) for Rupintrivir or 100mg/kg (n=10) for ribavirin; an equivalent volume of DMSO was injected in the control group (n=14). The Rupintrivir was injected every day for 10 days. Infected mice were monitored daily for signs of morbidity and mortality. The sickness of mice was evaluated using a graded score (0, healthy; 1, slow movement; 2, weakness in hind limbs; 3, paralysis in single limb; 4, paralysis in two limbs; and 5, death).

Dosage form

0.1mg/kg/day for 10 days; i.p.

Applications

Rupintrivir treatment effectively rescued EV71-induced paralysis and death in a suckling mouse model.

References:
[1] Rocha-Pereira J, Nascimento M S J, Ma Q, et al. The enterovirus protease inhibitor rupintrivir exerts cross-genotypic anti-norovirus activity and clears cells from the norovirus replicon[J]. Antimicrobial agents and chemotherapy, 2014, 58(8): 4675-4681.
[2] Zhang X, Song Z, Qin B, et al. Rupintrivir is a promising candidate for treating severe cases of enterovirus-71 infection: evaluation of antiviral efficacy in a murine infection model[J]. Antiviral research, 2013, 97(3): 264-269.

Produktdokumente (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
223537-30-2
Synonyme
AG7088
SMILES
O=C(C1=NOC(C)=C1)N[C@@H](C(C)C)C(C[C@@H](CC2=CC=C(F)C=C2)C(N[C@H](/C=C/C(OCC)=O)C[C@@H]3CCNC3=O)=O)=O
Summenformel
C31H39FN4O7
Molekulargewicht
598.66
Löslichkeit
DMSO : 50 mg/mL (83.52 mM; Need ultrasonic)
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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