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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 346629-30-9
- Formule: C31H29N3O5S2
- Masse moléculaire:587.71
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
|
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 |
Chemical Information
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CAS No. 346629-30-9
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Masse moléculaire 587.71
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Formule C31H29N3O5S2
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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
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Synonyms
L-454,560
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)