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.
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。
- 純度 : 99.55%
- CAS 番号: 185954-27-2
- 分子式: C18H21N5S
- 分子量:339.46
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
製品説明
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] |
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 185954-27-2
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性状 Solid
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分子量 339.46
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分子式 C18H21N5S
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SMILES
CCC1=NN(C2=C1CCN3C2=NN=C3C4=CC=CS4)C5CCCC5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
プロトコル
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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
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)