IRBM-Z-2
IRBM-Z-2 is a non-competitive, orally active Zika virus (ZIKV) NS2B-NS3 protease inhibitor, with IC50 values of 0.04 μM and 3.1 μM against the wild-type and I156T mutant strains, respectively. IRBM-Z-2 exhibits broad-spectrum anti-flavivirus potential, with IC50 values of 2.1 μM and 0.09 μM against the NS2B-NS3 proteases of dengue virus 2 (DENV2) and West Nile virus (WNV), respectively. IRBM-Z-1 inhibits ZIKV replication and alleviates virus-induced cytopathic effects. IRBM-Z-1 can be used in studies related to ZIKV infection.
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- No. CAS: 3014840-61-7
- Fòrmula: C22H18F3N7O2
- Peso molecular:469.42
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
In biochemical assays, IRBM-Z-2 inhibits the activity of the DENV2 NS2B-NS3T156I mutant protease with an IC50 of 0.4 μM, exhibiting stronger potency compared to the wild-type protease[1].
IRBM-Z-2 (72 h) potently inhibits the replication of wild-type Zika virus (ZIKV) replicons in Vero cells, with an EC50 of 0.03 μM, and no cytotoxicity is detected at concentrations up to 32 μM[1].
IRBM-Z-2 (72 h) inhibits the replication of ZIKV I156T mutant replicon in Vero cells, with an EC50 of 0.79 μM. No cytotoxicity is detected at concentrations up to 32 μM, and it exhibits a characteristic of reduced potency compared with the wild-type replicon[1].
IRBM-Z-2 (72 h) inhibits the replication of WNV replicons in Vero cells with an EC50 of 0.31 μM, and no cytotoxicity is detected at concentrations up to 32 μM[1].
IRBM-Z-2 (6 days) potently inhibits the cytopathic effect (CPE) induced by the ZIKV PRVABC59 strain in BHK-21 cells, with an EC50 of 0.016 μM, and no cytotoxicity is detected even at a concentration as high as 37.9 μM[1].
IRBM-Z-2 (48 h) inhibits the ZIKV Padova strain and H/PF/2013 strain in HuH-7 cells, with apparent IC50 values ranging from 6 to 20 nM, and no cytotoxicity is detected at the tested concentrations[1].
IRBM-Z-2 (6 days) inhibits the cytopathic effect (CPE) induced by West Nile virus strain Kern 515 in Vero76 cells, with an EC50 of 1.0 μM, and no cytotoxicity is detected at concentrations up to 50 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | CL | Vdss | T1/2 | Plasma Concentration | Cmax | AUC | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 6.1 mL/min/kg | 0.8 L/kg | 2.3 h | / | / | / | / |
| Rat[1] | 3 mg/kg | p.o. | / | / | / | / | 1.4 μM | 5.0 μM·h | 29 % |
| Rat[1] | 1 mg/kg | i.v. | 9.7 mL/min/kg | 1.4 L/kg | 2.8 h | / | / | / | / |
| Rat[1] | 3 mg/kg | p.o. | / | / | / | / | 1.6 μM | 4.0 μM·h | 90 % |
| Rat[1] | 100 mg/kg | i.p. | / | / | / | >1.39 μM | / | / | / |
| Rat[1] | 100 mg/kg | p.o. | / | / | / | >1.39 μM | 23.3 μM | 208 μM·h | / |
In Vivo
IRBM-Z-2 (100 mg/kg; oral gavage; twice daily; 14 consecutive days) reduces ZIKV serum viral load to undetectable levels by day 5, prevents ZIKV-induced weight loss, and results in 100% survival of AG129 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AG129 (male, 5 weeks old, IFNα/β and IFNγ receptors deficient)[1]
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Dosage:100 mg/kg
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Administration:intraperitoneally; once daily; 5 consecutive days
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Result:Reduced serum viral RNA levels by 3.6 log10 compared to untreated controls by day 1.
Reduced serum viral RNA levels by 4.5 log10 compared to untreated controls by the end of the 5-day study.
Fully protected mice from ZIKV-induced weight loss.
Showed no adverse clinical signs.
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Animal Model:AG129 (male, 5 weeks old, IFNα/β and IFNγ receptors deficient)[1]
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Dosage:100 mg/kg
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Administration:oral gavage; twice daily; 14 consecutive days
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Result:Reduced serum viral RNA levels by more than 6 log10 compared to vehicle-treated controls by day 3 post-infection.
Reduced serum viral RNA levels below the limit of detection by day 5, remaining undetectable through the end of the 14-day study.
Prevented ZIKV-induced weight loss.
Showed no adverse clinical signs.
Achieved 100% survival of treated mice over 14 days, compared to full mortality of vehicle controls by day 9.
Chemical Information
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No. CAS 3014840-61-7
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Peso molecular 469.42
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Fòrmula C22H18F3N7O2
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SMILES
O=C(NC1=CC=CC(C(F)(F)F)=C1)[N-]C2=C[N+](CC3=CC=C(C4=C(C)N=CN=C4C)C=N3)=NO2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IRBM-Z-2 Related Classifications
HY-181991 Related Classifications
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