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.
For research use only. We do not sell to patients.
- CAS No.: 346629-30-9
- Formula: C31H29N3O5S2
- Molecular Weight:587.71
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
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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Molecular Weight 587.71
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)