FGI-103
FGI-103 is a non-peptide filovirus inhibitor. FGI-103 has activity against Ebola virus (EBOV) and Marburg virus (MARV) infection, with EC50 values of 100 nM, 420 nM, 2.5 μM, and 2.5 μM against ZEBOV, SEBOV, MARV-Ravn, and MARV-Ci67, respectively. FGI-103 can be used for research on filovirus infection.
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- No. CAS: 907169-69-1
- Fòrmula: C19H16N6O
- Peso molecular:344.37
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
FGI-103 is a non-peptide filovirus inhibitor. FGI-103 has activity against Ebola virus (EBOV) and Marburg virus (MARV) infection, with EC50 values of 100 nM, 420 nM, 2.5 μM, and 2.5 μM against ZEBOV, SEBOV, MARV-Ravn, and MARV-Ci67, respectively. FGI-103 can be used for research on filovirus infection[1].
IC50 & Target
[1]|
ZEBOV 100 nM (EC50) |
SEBOV 420 nM (EC50) |
MARV-Ravn 2.5 μM (EC50) |
MARV-Ci67 2.5 μM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero E6 | CC50 |
≥ 50 μM
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Cytotoxicity against Vero E6 cells assessed as CC50 at or above 50 μM after 72 hrs by CellTiter Glo luminescence assay.
Cytotoxicity against Vero E6 cells assessed as CC50 at or above 50 μM after 72 hrs by CellTiter Glo luminescence assay.
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AAC.01315-09 |
| HEK-293T | CC50 |
≥ 50 μM
|
Cytotoxicity against HEK-293T cells assessed as CC50 at or above 50 μM after 72 hrs by CellTiter Glo luminescence assay.
Cytotoxicity against HEK-293T cells assessed as CC50 at or above 50 μM after 72 hrs by CellTiter Glo luminescence assay.
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AAC.01315-09 |
| MDCK | CC50 |
≥ 50 μM
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Cytotoxicity against MDCK cells assessed as CC50 at or above 50 μM after 72 hrs by CellTiter Glo luminescence assay.
Cytotoxicity against MDCK cells assessed as CC50 at or above 50 μM after 72 hrs by CellTiter Glo luminescence assay.
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AAC.01315-09 |
| A549 | CC50 |
≥ 50 μM
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Cytotoxicity against A549 cells assessed as CC50 at or above 50 μM after 72 hrs by CellTiter Glo luminescence assay.
Cytotoxicity against A549 cells assessed as CC50 at or above 50 μM after 72 hrs by CellTiter Glo luminescence assay.
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AAC.01315-09 |
| HEp-2 | CC50 |
≥ 50 μM
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Cytotoxicity against HEp-2 cells assessed as CC50 at or above 50 μM after 72 hrs by CellTiter Glo luminescence assay.
Cytotoxicity against HEp-2 cells assessed as CC50 at or above 50 μM after 72 hrs by CellTiter Glo luminescence assay.
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AAC.01315-09 |
In Vitro
Viral InfectionOthers
Viral Infection
FGI-103 (20 µM; overnight pretreatment-48 h post-infection) inhibits ZEBOV-GFP infection in Vero E6 cells in a dose-dependent manner[1].
FGI-103 (overnight pretreatment-incubation for 48 h) inhibits the replication of wild-type ZEBOV, SEBOV, MARV-Ravn, and MARV-Ci67 in the Vero E6 virus yield assay, with EC50 values of 100 nM, 420 nM, 2.5 μM, and 2.5 μM, respectively[1].
FGI-103 (overnight pretreatment-incubation for 48 h) inhibits the replication of wild-type ZEBOV, SEBOV, MARV-Ravn, and MARV-Ci67 in the Vero E6 virus yield assay, with EC50 values of 100 nM, 420 nM, 2.5 μM, and 2.5 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Viral InfectionCytokines & Chemokines
Viral Infection
FGI-103 (10 mg/kg; i.p.; administered 1 h before infection and on days 2 and 5 after infection; observed for 14 days) completely protects C57BL/6 mice against lethal mouse-adapted ZEBOV challenge[1].
FGI-103 (5-10 mg/kg; i.p.; administered once on day 1 post-infection; 14-day observation) exhibits activity in the C57BL/6 mouse model infected with the mouse-adapted ZEBOV strain, providing complete protection (100% survival in the 10 mg/kg group) or partial protection (60% survival in the 5 mg/kg group) of mice from lethal infection when administered therapeutically[1].
FGI-103 (5-10 mg/kg; i.p.; administered once on day 1 post-infection; 14-day observation) exhibits activity in the BALB/c mouse model infected with the mouse-adapted strain MARV-Ravn, providing complete protection (100% survival in the 10 mg/kg group) or partial protection (40% survival in the 5 mg/kg group) of mice against lethal Marburg virus challenge when administered therapeutically[1].
FGI-103 (5-10 mg/kg; i.p.; administered once on day 1 post-infection; 14-day observation) exhibits activity in the C57BL/6 mouse model infected with the mouse-adapted ZEBOV strain, providing complete protection (100% survival in the 10 mg/kg group) or partial protection (60% survival in the 5 mg/kg group) of mice from lethal infection when administered therapeutically[1].
FGI-103 (5-10 mg/kg; i.p.; administered once on day 1 post-infection; 14-day observation) exhibits activity in the BALB/c mouse model infected with the mouse-adapted strain MARV-Ravn, providing complete protection (100% survival in the 10 mg/kg group) or partial protection (40% survival in the 5 mg/kg group) of mice against lethal Marburg virus challenge when administered therapeutically[1].
Viral Infection
Cytokines & Chemokines
FGI-103 (10 mg/kg; i.p.; administered once on day 1 post-infection; days 2-8) delays viral appearance, reduces viral load in the kidney/liver/spleen and serum, inhibits pro-inflammatory cytokine secretion, lowers liver enzyme levels, and attenuates histopathological damage in the liver and spleen in the ZEBOV-infected C57BL/6 mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (8-10 weeks old) were established with a lethal infection
model via intraperitoneal (i.p.) injection of 1,000 PFU of mouse-adapted Zaire ebolavirus
(ZEBOV)[1] -
Dosage:10 mg/kg
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Administration:i.p.; day 0 (1 h before infection), day 2, and day 5 postinfection; 14 days
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Result:Vehicle-treated mice had 90% mortality.
Completely protected mice against lethal EBOV challenge (100% survival).
Transient overt signs of EBOV infection occurred in 5 of 10 mice beginning on day 8; all mice were healthy beginning 10 days after infection.
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Animal Model:C57BL/6 mice (8-10 weeks old) were established with a lethal infection
model via intraperitoneal (i.p.) injection of 1,000 PFU of mouse-adapted Zaire ebolavirus
(ZEBOV); BALB/c mice (8-12 weeks old) were established with a lethal infection model
via intraperitoneal injection of 1,000 PFU of mouse-adapted Marburg virus (MARV-Ravn)[1] -
Dosage:5 mg/kg;10 mg/kg
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Administration:i.p.; once at day 1 postinfection; 14 days
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Result:Completely protected mice infected with EBOV or MARV (100% survival), while
the 5 mg/kg dose provided 60% (EBOV) and 40% (MARV) protection rates, respectively.
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Animal Model:C57BL/6 mice (8-10 weeks old) were established with a lethal infection
model via intraperitoneal (i.p.) injection of 1,000 PFU of mouse-adapted Zaire ebolavirus
(ZEBOV)[1] -
Dosage:10 mg/kg
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Administration:i.p.; once at day 1 postinfection; 2, 4, 6, 8 days
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Result:Delayed the time at which the virus was detected in kidneys, liver, spleen, and serum.
Significantly reduced the viral load in tissues and serum, with titer levels often 1 to 2 logs (10- to 100-fold) lower than those in the control group.
Suppressed the cytokine storm, significantly lowering the levels of MCP-1 and IL-6 in the serum, which never reached the peak levels observed in the control group.
Protected liver function, significantly reducing the surge in concentrations of liver damage marker enzymes (ALT, AST, ALP) at day 6 postinfection.
Alleviated histopathological damage, mitigating hepatocellular necrosis in the liver and lymphocytolysis in the spleen, and restricted the widespread dissemination of viral antigens by day 6.
Related Protocols :
Chemical Information
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No. CAS 907169-69-1
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Peso molecular 344.37
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Fòrmula C19H16N6O
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SMILES
N=C(C1=CC=C2N=C(/C=C/C3=CC4=CC(C(N)=N)=CC=C4O3)NC2=C1)N
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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
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