Tofimilast
Tofimilast is an inhibitor of Phosphodiesterase 4 (PDE4) with an IC50 of 0.14 μM. Tofimilast exerts its anti-inflammatory effects by inhibiting the activity of PDE4, thereby increasing intracellular levels of cAMP.
For research use only. We do not sell to patients.
- CAS No.: 185954-27-2
- Formula: C18H21N5S
- Molecular Weight:339.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
PDE4 0.14 μM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
5.2 μM
Compound: 19, Tofimilast
|
Inhibition of human adenosine A1 receptor expressed in CHO cells
Inhibition of human adenosine A1 receptor expressed in CHO cells
|
[PMID: 17228876] |
| Monocyte | IC50 |
59 nM
Compound: 19, Tofimilast
|
Inhibition of LPS-stimulated TNF alpha release in human monocytes
Inhibition of LPS-stimulated TNF alpha release in human monocytes
|
[PMID: 17228876] |
| Monocyte | IC50 |
67 nM
Compound: 19, Tofimilast
|
Inhibition of PDE-mediated cAMP catabolism in human monocytes
Inhibition of PDE-mediated cAMP catabolism in human monocytes
|
[PMID: 17228876] |
| U-937 | EC50 |
230 nM
Compound: 19, Tofimilast
|
Increase in cAMP levels in PGE1-stimulated U937 cells
Increase in cAMP levels in PGE1-stimulated U937 cells
|
[PMID: 17228876] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 185954-27-2
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Molecular Weight 339.46
-
Formula C18H21N5S
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SMILES
CCC1=NN(C2=C1CCN3C2=NN=C3C4=CC=CS4)C5CCCC5
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Shipping
Room temperature in continental US; may vary elsewhere.
-
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)