GHP-88310
GHP-88310 is an orally active broad-spectrum paramyxovirus and orthomyxovirus inhibitor that targets the L protein-RdRP complex, and exhibits activity against respiratory viruses and viruses of the genus Morbillivirus. GHP-88310 binds to the central cavity of the polymerase protein, blocks replicase and transcriptase activities, interferes with the viral life cycle and inhibits viral replication. GHP-88310 can be used in studies of paramyxovirus infections, including morbillivirus-like diseases, human parainfluenza virus type 3 infection and measles.
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- 화학식: C16H14N4O
- 분자량:278.31
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All DNA/RNA Synthesis Isoforms
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Biological Activity
GHP-88310 (80 μM; 2 h) displays high plasma-membrane permeability, reaching an intracellular exposure plateau of approximately 105 pmol per 106 cells within 15 minutes of wash-in in undifferentiated human bronchial tracheal epithelial cells (HBTECs)[2].
GHP-88310 (50 μM) shows submicromolar potency and a steep Hill slope against HPIV3 in undifferentiated HBTECs, with fully sterilizing efficacy at concentrations of 10 μM and above[2].
GHP-88310 (0-200 μM; 48 h) is well tolerated in well-differentiated human airway epithelium organoids at the highest physiologically achievable concentrations without disturbing tissue integrity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GHP-88310 (100-150 mg/kg; oral administration; twice daily) yields a 100% survival rate in ferrets exposed to canine distemper virus via air, and the twice-daily dosing regimen achieves complete blockage of transmission[1].
GHP-88310 (150 mg/kg; p.o.; twice daily) results in 100% survival of ferret source animals infected with canine distemper virus, blocks virus transmission from these source animals to contact ferrets, and shortens the infectious period of the source animals by 5 days[1].
GHP-88310 (150 mg/kg; p.o.; twice daily; 7.5 days) confers 100% survival rate in SeV-infected 129X1/SvJ mice and significantly reduces their respiratory viral load[2].
GHP-88310 (16.5-150 mg/kg; p.o.; twice daily, once daily; for 3 consecutive days) exhibits potent anti-HPIV3 activity in cotton rats, and significantly reduces viral loads at doses as low as 16.5 mg/kg twice daily or 150 mg/kg once daily[2].
GHP-88310 (50-150 mg/kg; p.o.; twice daily, once daily; 7-18 days) achieves 100% survival in ferrets with lethal CDV-induced measles-like disease, reduces viremia and viral shedding levels, and alleviates lymphopenia; at a dose of 150 mg/kg twice daily, the drug exhibits sterilizing efficacy[2].
GHP-88310 (300-1200 mg/kg; p.o.; twice daily; 7 days) is well tolerated by cotton rats at daily doses up to 2400 mg/kg, with plasma exposure showing a positive correlation with dose[2].
GHP-88310 (50-1000 mg/kg; p.o.; twice daily; for 7 consecutive days) is well tolerated in ferrets even at a daily dose of up to 2000 mg/kg, with plasma exposure proportional to the dose, and no hematological or clinical adverse reactions are detected[2].
GHP-88310 (50-500 mg/kg; p.o.; single administration) is well tolerated in beagle dogs, with plasma exposure showing a dose-dependent pattern[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mustela putorius furo (female, 3-5 months old)[1]
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Dosage:150 mg/kg
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Administration:p.o.; twice daily
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Result:Kept all treated contact ferrets disease-free for the entire study duration.
Eliminated detectable viraemia or virus in nasal lavages.
Caused no changes in complete blood count profiles.
Enabled 2 of 3 treated ferrets to mount a protective neutralizing antibody response approximately 3 weeks after co-housing.
Achieved 100% survival of treated ferrets, while all vehicle-treated contacts succumbed by study day 19.
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Animal Model:Mustela putorius furo (female, 3-5 months old)[1]
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Dosage:100 mg/kg; 150 mg/kg
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Administration:p.o.; twice daily
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Result:Achieved 100% survival of all treated sentinels after initial airborne exposure, while all vehicle-treated sentinels succumbed by study day 21.
Kept ferrets receiving twice-daily regimens disease-free with no lymphocytopaenia.
Resulted in transient mild viraemia but no detectable virus in nasal lavages for the 6-day post-contact twice-daily group.
Caused minor, transient clinical signs, moderate transient viraemia, and low-level virus shedding (1-2 orders of magnitude lower than vehicle controls) in the once-daily prophylactic group.
Induced sterilizing immunity (no neutralizing antibodies, all succumbed to rechallenge) in prophylactic and 3-day post-contact twice-daily groups.
Enabled the once-daily group and 2 of 3 ferrets in the 6-day post-contact twice-daily group to mount robust neutralizing antibody responses and survive rechallenge.
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Animal Model:Mustela putorius furo (female, 3-5 months old)[1]
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Dosage:150 mg/kg
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Administration:p.o.; twice daily
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Result:Achieved 100% survival of source ferrets treated at 4 or 6 d.p.i., with only transient viraemia and minimal virus shedding.
Enabled 2 of 3 ferrets treated at 8 d.p.i. to survive.
Resulted in 100% survival of all direct and airborne contact ferrets of treated sources, with no clinical signs, no lymphocytopaenia, and no neutralizing antibodies.
Caused all airborne contacts of vehicle-treated sources to succumb by study day 25.
Shortened the contagious phase of sources by 5 days compared to vehicle controls.
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Animal Model:129X1/SvJ mice[2]
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Dosage:150 mg/kg
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Administration:p.o.; twice daily; 7.5 days
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Result:Achieved 100% survival without development of clinical signs.
Significantly reduced viral load in the upper and lower respiratory tract compared to vehicle-treated mice.
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Animal Model:Cotton rats (female, aged 3-4 weeks, Envigo)[2]
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Dosage:16.5 mg/kg; 50 mg/kg; 150 mg/kg
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Administration:p.o.; twice daily; 3 days
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Result:Achieved lowest efficacious dose of 50 mg/kg b.i.d. for upper respiratory tract viral load reduction.
Achieved lowest efficacious dose of 16.5 mg/kg b.i.d. for lower respiratory tract viral load reduction.
Significantly reduced viral load in trachea and lower respiratory tract at 150 mg/kg q.d. or higher without changes in body weight or temperature.
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Animal Model:Ferrets (unvaccinated female, aged 8 months, Triple F Farms)[2]
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Dosage:50 mg/kg; 100 mg/kg; 150 mg/kg
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Administration:p.o.; b.i.d.; 7-18 days
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Result:Achieved 100% survival of lethal infection with full mitigation of clinical signs, while all vehicle-treated ferrets succumbed (median survival 11 dpi).
Lowered peak PBMC-associated viremia titers by ~1 order of magnitude and resolved viremia by 15-16 dpi at 50 or 100 mg/kg q.d. or 50 mg/kg b.i.d.
Reduced peak viremia by 2 orders of magnitude and achieved sterilization at 10 dpi at 150 mg/kg b.i.d.
Reduced peak nasal virus shedding by 2 orders of magnitude compared to vehicle controls and ceased shedding by 6 dpi at 150 mg/kg b.i.d.; resolved shedding by 17 dpi in other treated groups.
Fully suppressed lymphocytopenia at 150 mg/kg b.i.d., efficiently mitigated lymphocytopenia at 50 mg/kg b.i.d. or 100 mg/kg q.d., and resulted in transient lymphocytopenia (resolving by 27 dpi) at 50 mg/kg q.d.
Detected no polymerase mutations via whole genome sequencing of virus populations from treated animals, indicating a high barrier to viral escape.
Chemical Information
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Appearance Solid
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분자량 278.31
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화학식 C16H14N4O
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Color Off-white to gray
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SMILES
CNC1=CC=CC(C2=CN=CC3=C2C=CN=C3)=C1C(N)=O
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Synonyms
EIDD-3608
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 0.5 mg/mL (1.80 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (287 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Lieber CM, et al. Antiviral GHP-88310 blocks contact-mediated and airborne transmission in a ferret model of measles-like disease. Nature microbiology. 2026 Jul 24. [Content Brief]
[2]. Lieber CM, et al. Developmental candidate GHP-88310/EIDD-3608 with high tolerability and oral efficacy in measles and respiratory paramyxovirus models. Science advances. 2026 May 22;12(21):eaef1594. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5931 mL | 17.9656 mL | 35.9312 mL | 89.8279 mL |
- GHP-88310
- EIDD-3608
- GHP88310
- GHP 88310
- EIDD3608
- EIDD 3608
- DNA/RNA Synthesis
- Measles Virus
- 129X1/SvJ mice
- respiroviruses
- SeV
- orthoparamyxovirus polymerase (L) protein
- canine distemper virus
- RNA-dependent RNA polymerase (RdRP) complex
- morbilliviruses
- human parainfluenza virus type-3
- ferrets
- human airway epithelium organoids
- Inhibitor
- inhibitor
- inhibit