Ro 13-3978
Ro 13-3978 is an orally active antischistosomal agent. Ro 13-3978 exhibits excellent in vivo antischistosomal activity against juvenile and adult Schistosoma mansoni infections. Ro 13-3978 shows no in vivo activity against E. caproni and F. hepatica. Ro 13-3978 blocks dihydrotestosterone-induced proliferation of androgen-dependent cells. Ro 13-3978 can be used in research related to schistosomiasis.
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: 70842-04-5
- 分子式: C12H10F4N2O2
- 分子量:290.22
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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
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Schistosome |
Ro 13-3978 (100 μg/mL; 72 h) moderately reduces the motility of newly transformed S. mansoni schistosomula in vitro without causing tegument damage[1].
Ro 13-3978 (0.12-90 μM; 70 h) shows no cytotoxicity against rat skeletal myoblast L6 cells at concentrations up to 90 μM after 70 h of incubation, with an IC50 greater than 90 μM[1].
Ro 13-3978 (25-100 μg/mL; 72 h) causes mild tegumentary changes in adult S. mansoni worms in vitro, including wrinkling in males and sloughing in a subset of females[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | AUC0-last |
|---|---|---|---|---|
| Mice[2] | 100 mg/kg | p.o. | 124 μM | 2740 μM·h |
Ro 13-3978 (100 mg/kg; p.o.; single dose) shows stage-specific antischistosomal activity in NMRI mice, with high efficacy (64.3-94.6% total WBR) against S. mansoni from day 22 post-infection onwards, no activity against 7-14 day-old worms, and moderate efficacy when administered pre-infection[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRI mice (female, weight ~20-22 g, orally infected with Schistosoma mansoni cercariae)[1]
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Dosage:12.5-100 mg/kg (adult infections); 50-200 mg/kg (juvenile infections)
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Administration:p.o.; single dose
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Result:Reduced total adult S.
mansoni worm burden by 37.1%, 82.6%, 78.2%, and 94.6% at 12.5 mg/kg, 25 mg/kg, 50 mg/kg, and 100 mg/kg respectively.
Reduced female adult S.
mansoni worm burden by 33.8%, 84.5%, 57.3%, and 88.0% at 12.5 mg/kg, 25 mg/kg, 50 mg/kg, and 100 mg/kg respectively.
Calculated an ED50 of 14.6 mg/kg for 49 day-old S. mansoni infections.
Reduced total juvenile S.
mansoni worm burden by 0%, 63.8%, and 88.1% at 50 mg/kg, 100 mg/kg, and 200 mg/kg respectively.
Reduced female juvenile S.
mansoni worm burden by 0%, 57.3%, and 85.4% at 50 mg/kg, 100 mg/kg, and 200 mg/kg respectively.
Calculated an ED50 of 138.9 mg/kg for 22 day-old S. mansoni infections.
化学情報
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CAS 番号 70842-04-5
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分子量 290.22
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分子式 C12H10F4N2O2
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SMILES
O=C1NC(C(=O)N1C2=CC=C(F)C(=C2)C(F)(F)F)(C)C
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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)
Ro 13-3978 関連分類
HY-W054427 関連分類
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