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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1222509-12-7
- 分子式: C15H10BF4NO3
- 分子量:339.05
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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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
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[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] |
化学情報
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CAS 番号 1222509-12-7
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分子量 339.05
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)