S-8660
S-8660 is an orally active, selective inhibitor of dihydroorotate dehydrogenase (DHODH). As an antiproliferative prodrug and an analog of Brequinar (HY-108325), S-8660 exhibits immunosuppressive activity. Its effect on prolonging cardiac allograft survival is enhanced when used in combination with Cyclosporin A (HY-B0579). S-8660 can be used in studies of cardiac transplant rejection.
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- CAS No.: 96201-52-4
- Formule: C23H16ClNO2
- Masse moléculaire:373.83
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
S-8660 selectively inhibits mitochondrial dihydroorotate dehydrogenase, disrupting de novo pyrimidine synthesis in a cell-free biochemical system[1].
S-8660 suppresses human mixed-lymphocyte responses in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ACI (RT1a) donors; Lewis (RT11) recipients[1]
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Dosage:5 mg/kg; 20 mg/kg
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Administration:p.o.; once daily; starting 2 days pre-transplant for up to 30 days post-transplant
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Result:Extended cardiac allograft survival in a dose-dependent manner.
Achieved a median graft survival time of 32 days with the tapered dose regimen, compared to control median survival of 7 days.
Chemical Information
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CAS No. 96201-52-4
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Masse moléculaire 373.83
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Formule C23H16ClNO2
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SMILES
O=C(O)C1=C(C(C2=CC=C(C=C2)C3=CC=CC=C3)=NC4=CC=CC(Cl)=C14)C
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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)
- S-8660
- 96201-52-4
- S8660
- S 8660
- Dihydroorotate Dehydrogenase
- delayed-type hypersensitivity
- antiproliferative prodrug
- immunosuppressive activity
- cardiac allograft rejection
- dihydroorotate dehydrogenase
- cardiac allograft survival
- de novo pyrimidine synthesis
- rats
- cyclosporine
- human mixed-lymphocyte responses
- Inhibitor
- inhibitor
- inhibit