MK-0359
MK-0359 (L-454,560) is a selective and orally active PDE4 inhibitor, and can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
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: 346629-30-9
- 分子式: C31H29N3O5S2
- 分子量:587.71
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
49.9 μM
Compound: 3
|
Displacement of [35S]MK-499 from human ERG expressed in HEK293 cells
Displacement of [35S]MK-499 from human ERG expressed in HEK293 cells
|
[PMID: 18835163] |
| Sf21 | IC50 |
3.9 μM
Compound: 4, L-454560
|
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB2 expressed in baculovirus infected insect Sf21 cells
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB2 expressed in baculovirus infected insect Sf21 cells
|
[PMID: 22023548] |
| Sf21 | IC50 |
8.8 μM
Compound: 4, L-454560
|
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells
|
[PMID: 22023548] |
| Sf9 | IC50 |
1.4 nM
Compound: 3
|
Intrinsic inhibition of GST-fused human PDE4A expressed in SF9 cells
Intrinsic inhibition of GST-fused human PDE4A expressed in SF9 cells
|
[PMID: 18835163] |
| Sf9 | IC50 |
3 nM
Compound: 1, L-454560
|
Inhibition of PDE4 expressed in SF9 cells
Inhibition of PDE4 expressed in SF9 cells
|
[PMID: 18207397] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 346629-30-9
-
分子量 587.71
-
分子式 C31H29N3O5S2
-
SMILES
O=S(C1=CC=C(/C(C2=NC(C)=NO2)=C\C3=CC(C4=C5N=CC=CC5=CC(C(S(=O)(C)=O)(C)C)=C4)=CC=C3)C=C1)(C)=O
-
別名
L-454,560
-
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)