WEHI-P8
Based on 1 Customer Validation
WEHI-P8 is an orally active SARS-CoV-2 papain-like protease (PLpro) inhibitor with an IC50 of 12 nM and a Kd of 9.0 nM. WEHI-P8 reduces viral load, body weight loss, pulmonary inflammation, immune cell infiltration and pro-inflammatory mediator levels in SARS-CoV-2-infected mice. WEHI-P8 prevents pulmonary hemorrhage, immune cell infiltration, fibrotic remodeling and neuroinflammation, and improves cognitive function in a mouse model of post-acute sequelae of SARS-CoV-2 infection (PASC). WEHI-P8 is applicable for the research of COVID-19 and PASC.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.03%
- 화학식: C25H34N2O3
- 분자량:410.55
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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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
WEHI-P8 (16-24 h) inhibits the activity of SARS-CoV-2 PLpro in FRET assays using HEK293T cells, with an EC50 of 298 nM[1].
WEHI-P8 (0-5 μM) inhibits SARS-CoV-2 replication in Vero cells in plaque assays, with an antiviral EC50 of 360 nM, which slightly decreases to 290 nM when combined with a P-glycoprotein inhibitor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Cmax | Tmax |
|---|---|---|---|---|---|
| Mice[1] | 100 mg/kg | p.o. | 14 h | 7.07 μM | 1 h |
WEHI-P8 (150 mg/kg; p.o.; administered 2 h before infection, 6 h after infection, and 24 h after infection) prevents acute infection-induced mortality, alleviates long-term pulmonary pathological damage, mitigates neuroinflammation, and improves cognitive function in a PASC 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 J (WT, 6-8 weeks old, both sexes, intranasal infection with mouse-adapted SARS-CoV-2 P21 strain)[1]
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Dosage:100 mg/kg; 150 mg/kg
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Administration:p.o.; 6 h, 24 h, 48 h post-infection
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Result:Reduced lung viral burden.
Prevented infection-induced weight loss.
Reduced lung haemorrhage and inflammation to mild levels (100 mg/kg) or minimal/unremarkable levels (150 mg/kg).
Significantly reduced lung macrophage and neutrophil counts (100 mg/kg); significantly reduced lung macrophage, neutrophil, and T cell counts (150 mg/kg).
Significantly reduced lung levels of multiple pro-inflammatory cytokines/chemokines including IFN-γ, IL-1β, TNF, IL-18, IL-6, GROα, and MCP-1.
Reduced lung viral burden to levels below the lower limit of detection (150 mg/kg).
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Animal Model:C57BL/6 J (WT, 11-12 weeks old, both sexes, intranasal infection with mouse-adapted SARS-CoV-2 P21 strain)[1]
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Dosage:150 mg/kg
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Administration:p.o.; 2 h pre-infection, 6 h post-infection, 24 h post-infection
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Result:Ensured 100% survival of treated mice during the acute infection phase, compared to vehicle-treated mice requiring euthanasia.
Prevented infection-induced weight loss during the acute phase.
Reduced lung haemorrhage and inflammatory foci to near-unremarkable levels, with lungs histologically similar to mock-infected mice.
Significantly reduced microglial activation (increased microglial projection area) in the hippocampus, indicating reduced neuroinflammation.
Significantly increased time spent exploring a novel object in the Novel Object Recognition Test, indicating improved cognitive function compared to vehicle and PLT-treated mice.
Rescued the infection-induced reduction in total distance travelled during behavioural testing in female mice, a deficit not mitigated by PLT treatment.
Chemical Information
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Appearance Solid
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분자량 410.55
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화학식 C25H34N2O3
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Color White to off-white
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SMILES
CCO/N=C([C@@H]1CCCN(C1)[C@H]2CC[C@H](CC2)O)/C3=CC4=C(C=C(C=C4)OC)C=C3
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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 : 100 mg/mL (243.58 mM; Need ultrasonic; 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 (275 KB)
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SDS (252 KB)
- English - EN (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
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 | 2.4358 mL | 12.1788 mL | 24.3576 mL | 60.8939 mL |
| 5 mM | 0.4872 mL | 2.4358 mL | 4.8715 mL | 12.1788 mL | |
| 10 mM | 0.2436 mL | 1.2179 mL | 2.4358 mL | 6.0894 mL | |
| 15 mM | 0.1624 mL | 0.8119 mL | 1.6238 mL | 4.0596 mL | |
| 20 mM | 0.1218 mL | 0.6089 mL | 1.2179 mL | 3.0447 mL | |
| 25 mM | 0.0974 mL | 0.4872 mL | 0.9743 mL | 2.4358 mL | |
| 30 mM | 0.0812 mL | 0.4060 mL | 0.8119 mL | 2.0298 mL | |
| 40 mM | 0.0609 mL | 0.3045 mL | 0.6089 mL | 1.5223 mL | |
| 50 mM | 0.0487 mL | 0.2436 mL | 0.4872 mL | 1.2179 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4060 mL | 1.0149 mL | |
| 80 mM | 0.0304 mL | 0.1522 mL | 0.3045 mL | 0.7612 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2436 mL | 0.6089 mL |
WEHI-P8 Related Classifications
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