CWHM-117
CWHM-117 is an orally active aspartic protease inhibitor with selective activity against Toxoplasma gondii. CWHM-117 inhibits the proliferation of Toxoplasma gondii tachyzoites in human fibroblasts, with an EC50 of 2.00 µM. CWHM-117 delays mortality in an acute mouse model of toxoplasmosis. In a chronic mouse model of toxoplasmosis, CWHM-117 reduces brain cyst burden and prolongs survival. CWHM-117 can be used for research on toxoplasmosis.
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- CAS No.: 1505452-80-1
- Formule: C23H27N3O3
- Masse moléculaire:393.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
Toxoplasma 2 μM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HFF | EC50 |
2.00 μM
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Inhibition of intracellular Toxoplasma gondii RH-2F1 tachyzoite proliferation in human foreskin fibroblasts (HFF) incubated for 72 h post-infection, measured by β-galactosidase activity using chlorophenol red-β-D-galactopyranoside (CPRG) as substrate.
Inhibition of intracellular Toxoplasma gondii RH-2F1 tachyzoite proliferation in human foreskin fibroblasts (HFF) incubated for 72 h post-infection, measured by β-galactosidase activity using chlorophenol red-β-D-galactopyranoside (CPRG) as substrate.
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PMC13435739 |
| HFF | CC50 |
14.30 μM
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Cytotoxicity against human foreskin fibroblasts (HFF) incubated for 72 h, assessed by cell viability measured via resazurin assay.
Cytotoxicity against human foreskin fibroblasts (HFF) incubated for 72 h, assessed by cell viability measured via resazurin assay.
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PMC13435739 |
In Vitro
CWHM-117 (0.39-100 μM; 72 h) potently inhibits intracellular proliferation of T. gondii RH-2F1 tachyzoites in HFF cells with an EC50 of 2.00 μM[1].
CWHM-117 (0.39-100 μM; 72 h) has a CC50 of 14.30 μM against HFF cells, with a selectivity index of 7.15 for T. gondii tachyzoites[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CWHM-117 (150 mg/kg/day; p.o.; once daily; 5 consecutive days) significantly reduces cerebral cyst burden in a murine chronic toxoplasmosis model, demonstrating activity against the latent bradyzoite stage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss mice (5-6 week old) were infected intraperitoneally with 2 × 105 freshly egressed T. gondii tachyzoites (RH strain)[1]
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Dosage:150 mg/kg/day
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Administration:p.o.; once daily; 10 consecutive days
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Result:Delayed mortality, with treated animals surviving up to day 11 post-infection compared to vehicle-treated animals that succumbed between days 7 and 9 post-infection.
Showed no significant weight loss compared to the vehicle group.
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Animal Model:Swiss mice (5-6 week old) were orally infected with 10 brain cysts of T. gondii (ME-49 strain)[1]
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Dosage:150 mg/kg/day
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Administration:p.o.; once daily; 5 consecutive days
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Result:Caused a marked, statistically significant reduction in the number of brain cysts compared to the vehicle-treated group.
Chemical Information
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CAS No. 1505452-80-1
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Masse moléculaire 393.48
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Formule C23H27N3O3
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SMILES
N=C(NC1(C2=CC=C(OC)C=C2)C3=CC=C(OC)C=C3)N(C4CCCCC4)C1=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CWHM-117 Related Classifications
HY-188134 Related Classifications
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