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.
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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
|
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 |
化学情報
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CAS 番号 185954-27-2
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性状 Solid
-
分子量 339.46
-
分子式 C18H21N5S
-
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
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)