Rupintrivir
Catalog No.: GC50441Purity:>98.00%Synonyms: AG7088
Rupintrivirvr (AG7088), un fÁrmaco antiviral, es un inhibidor potente, selectivo e irreversible de la proteasa 3C del rinovirus humano (HRV).
Los productos son exclusivamente para uso en investigación. No aptos para uso humano. No vendemos a pacientes.
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 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citas (Citations)
1 publicationsPublicaciones de investigadores que utilizan este productoDescripción (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.
Protocolo (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: | |
Documentos del producto (Product Documents)
Purity:>98.00%Appearance:A solid
Propiedades químicas (Chemical Properties)
N.º CAS
223537-30-2
Sinónimos
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
Fórmula molecular
C31H39FN4O7
Peso molecular
598.66
Solubilidad
DMSO : 50 mg/mL (83.52 mM; Need ultrasonic)
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.
Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad
g/mol
Reviews
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