Tofimilast
Based on 1 Customer Validation
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.
- Purity : 99.55%
- CAS No.: 185954-27-2
- Formula: C18H21N5S
- Molecular Weight:339.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
IC50 & Target
|
PDE4 0.14 μM (IC50) |
Cellular Effect
|
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] |
Clinical Trial
| 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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Appearance Solid
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Molecular Weight 339.46
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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.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)