1. Anti-infection
  2. Parasite
  3. 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.

For research use only. We do not sell to patients.

Ro 13-3978

Ro 13-3978 Chemical Structure

CAS No. : 70842-04-5

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Description

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[1][2].

IC50 & Target[1]

Schistosome

 

In Vitro

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.

Parmacokinetics
Species Dose Route Cmax AUC0-last
Mice[2] 100 mg/kg p.o. 124 μM 2740 μM·h
In Vivo

Ro 13-3978 (12.5-200 mg/kg; p.o.; single dose) exhibits dose-dependent antischistosomal activity in NMRI mice, with an ED50 of 14.6 mg/kg against adult S. mansoni and 138.9 mg/kg against juvenile S. mansoni following a single oral dose[1].
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.

Animal Model: NMRI mice (female, weight ~20-22 g, orally infected with Schistosoma mansoni cercariae)[1]
Dosage: 12.5-100 mg/kg (adult infections); 50-200 mg/kg (juvenile infections)
Administration: p.o.; single dose
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.
Molecular Weight

290.22

Formula

C12H10F4N2O2

CAS No.
SMILES

O=C1NC(C(=O)N1C2=CC=C(F)C(=C2)C(F)(F)F)(C)C

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Ro 13-3978
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HY-W054427
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