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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1505452-80-1
- 分子式: C23H27N3O3
- 分子量:393.48
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
IC50 & Target
[1]|
Toxoplasma 2 μM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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 |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 1505452-80-1
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分子量 393.48
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CWHM-117 関連分類
HY-188134 関連分類
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