Rupintrivir
Catalog No.: GC50441Purity:>98.00%Synonyms: AG7088
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.
Products are for research use only. Not for human use. We do not sell to patients.
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
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $246.00 | In Stock | 1 | |
| 1mg | $82.00 | In Stock | 1 | |
| 5mg | $186.00 | In Stock | 1 | |
| 10mg | $311.00 | In Stock | 1 | |
| 25mg | $494.00 | In Stock | 1 | |
| 50mg | $673.00 | In Stock | 1 | |
| 100mg | $888.00 | In Stock | 1 |
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Citations
1 publicationsPublications from researchers using this productDescription
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.
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: | |
Product Documents
Purity:>98.00%Appearance:A solid
Chemical Properties
CAS No.
223537-30-2
Synonyms
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
Molecular Formula
C31H39FN4O7
Molecular Weight
598.66
Solubility
DMSO : 50 mg/mL (83.52 mM; Need ultrasonic)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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