SCYX-6759
SCYX-6759 is an orally active, blood-brain barrier permeable anti-T. brucei agent. SCYX-6759 inhibits cytochrome P450 (IC50s: 30.3, 30.6, 47.4 μM for 2D6, 2C9, 2C19, respectively.) SCYX-6759 exhibits potent activity against T. b. brucei 427, T. b. rhodesiense STIB900, and T. b. gambiense STIB930, with IC50s of 0.07, 0.038 and 0.030 μg/mL, respectively.
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- CAS. Nr.: 1222509-12-7
- Formel: C15H10BF4NO3
- Molecular Weight:339.05
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Speicherung:
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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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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CYP2D6 30.3 μM (IC50) |
CYP2C9 30.6 μM (IC50) |
CYP2C19 47.4 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MRC5 | CC50 |
>64 μM
Compound: 3; SCYX-6759
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Cytotoxicity against human MRC5 cells measured after 3 days by resazurin staining based fluorometric analysis
Cytotoxicity against human MRC5 cells measured after 3 days by resazurin staining based fluorometric analysis
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[PMID: 34711050] |
| PBMC | IC50 |
13 μM
Compound: 1L
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Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
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[PMID: 24075731] |
| PBMC | IC50 |
3.2 μM
Compound: 1L
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Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-1beta release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-1beta release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
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[PMID: 24075731] |
| PBMC | IC50 |
5.6 μM
Compound: 1L
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Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-6 release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-6 release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
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[PMID: 24075731] |
| Peritoneal macrophage | CC50 |
>64 μM
Compound: 3; SCYX-6759
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Cytotoxicity against mouse primary peritoneal macrophages measured after 3 days by resazurin staining based fluorometric analysis
Cytotoxicity against mouse primary peritoneal macrophages measured after 3 days by resazurin staining based fluorometric analysis
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[PMID: 34711050] |
Chemical Information
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CAS. Nr. 1222509-12-7
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Molecular Weight 339.05
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Formel C15H10BF4NO3
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SMILES
O=C(C1=CC=C(C=C1C(F)(F)F)F)NC2=CC=C3C(B(OC3)O)=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
SCYX-6759 Related Classifications
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