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.
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- CAS No.: 70842-04-5
- 화학식: C12H10F4N2O2
- 분자량:290.22
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보관:
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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Biological Activity
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Chemical Information
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Biological Activity
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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.
Chemical Information
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CAS No. 70842-04-5
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분자량 290.22
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ro 13-3978 Related Classifications
HY-W054427 Related Classifications
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