S-8660
S-8660 is an orally active and selective inhibitor of dihydroorotate dehydrogenase (DHODH). S-8660 is an analog of Brequinar (HY-108325) and exhibits immunosuppressive activity. When combined with Cyclosporin A (HY-B0579), it enhances the effect of prolonging cardiac allograft survival. S-8660 can be used for research on cardiac transplant rejection.
For research use only. We do not sell to patients.
- CAS No.: 96201-52-4
- Formula: C23H16ClNO2
- Molecular Weight:373.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
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. .
In Vivo
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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Molecular Weight 373.83
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- 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