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 No.: 1222509-12-7
- 화학식: C15H10BF4NO3
- 분자량:339.05
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Parasite Isoforms
More
Biological Activity
|
CYP2D6 30.3 μM (IC50) |
CYP2C9 30.6 μM (IC50) |
CYP2C19 47.4 μM (IC50) |
|
Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MRC5 | CC50 |
>64 μM
Compound: 3; SCYX-6759
|
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
|
[PMID: 34711050] |
| PBMC | IC50 |
13 μM
Compound: 1L
|
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
|
[PMID: 24075731] |
| PBMC | IC50 |
3.2 μM
Compound: 1L
|
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
|
[PMID: 24075731] |
| PBMC | IC50 |
5.6 μM
Compound: 1L
|
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
|
[PMID: 24075731] |
| Peritoneal macrophage | CC50 |
>64 μM
Compound: 3; SCYX-6759
|
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
|
[PMID: 34711050] |
Chemical Information
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CAS No. 1222509-12-7
-
분자량 339.05
-
화학식 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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선적
Room temperature in continental US; may vary elsewhere.
-
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)