Tanimilast
Based on 1 Customer Validation
Tanimilast (CHF-6001) is an orally active and selective phosphodiesterase 4 inhibitor (IC50=0.026 nM) with robust anti-inflammatory activity and suitable for topical pulmonary administration. Tanimilast increases cellular cAMP levels, and inhibits NF-κB signaling pathway. Tanimilast is used for the research of obstructive lung diseases.
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: 99.71%
- CAS 番号: 1239278-59-1
- 分子式: C30H30Cl2F2N2O8S
- 分子量:687.54
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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
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
PDE4 0.026 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-937 | IC50 |
0.04 nM
Compound: (S)-32a
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Inhibition of PDE4 isolated from human U937 cells assessed as reduction in cAMP level by LANCE assay
Inhibition of PDE4 isolated from human U937 cells assessed as reduction in cAMP level by LANCE assay
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[PMID: 24400806] |
体外実験
Tanimilast (0.1 nM-0.1 μM, 24 h) increases the expression of CCR7 protein; inhibits the production of cytokines such as TNF-α, IL-1β, IL-6, IL-12, and IL-23; reduces the production of chemokines such as CXCL8, CCL3, CXCL10, and CCL19, IC50s in LPS (HY-D1056)-stimulated human monocyte-derived dendritic cells are 0.5, 4.6, 2.8, 1.7, 9.3, 7.2, 1.2, 1.8 and 0.8 nM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human monocyte-derived dendritic cells
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Concentration:0.1 nM-0.1 μM
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Incubation Time:24 h
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Result:Inhibited the expression of TNF-α and CXCL8.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS (HY-D1056)-induced acute pulmonary inflammation in mouse models[3]
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Dosage:100-600 µg/kg
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Administration:dry powder inhalation, single dose
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Result:Reduced the number of white blood cells (WBC) and neutrophils in bronchoalveolar lavage fluid (BALF).
Reduced the concentrations of proinflammatory cytokines, such as TNF-α, G-CSF, IL-1β, and RANTES in BALF.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1239278-59-1
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性状 Solid
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分子量 687.54
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分子式 C30H30Cl2F2N2O8S
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Color White to off-white
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SMILES
O=C(O[C@H](C1=CC=C(OC(F)F)C(OCC2CC2)=C1)CC3=C(Cl)C=[N+]([O-])C=C3Cl)C4=CC=C(NS(=O)(C)=O)C(OCC5CC5)=C4
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別名
CHF-6001
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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
溶剤 & 溶解度
体外:
DMSO : 200 mg/mL (290.89 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (282 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Moretto N, et al., CHF6001 I: a novel highly potent and selective phosphodiesterase 4 inhibitor with robust anti-inflammatory activity and suitable for topical pulmonary administration. J Pharmacol Exp Ther. 2015 Mar;352(3):559-67. [Content Brief]
[2]. Gianello V, et al., The PDE4 inhibitor CHF6001 modulates pro-inflammatory cytokines, chemokines and Th1- and Th17-polarizing cytokines in human dendritic cells. Biochem Pharmacol. 2019 May;163:371-380. [Content Brief]
[3]. Stellari FF, et al., CHF6001 Inhibits NF-κB Activation and Neutrophilic Recruitment in LPS-Induced Lung Inflammation in Mice. Front Pharmacol. 2019 Nov 12;10:1337. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4545 mL | 7.2723 mL | 14.5446 mL | 36.3615 mL |
| 5 mM | 0.2909 mL | 1.4545 mL | 2.9089 mL | 7.2723 mL | |
| 10 mM | 0.1454 mL | 0.7272 mL | 1.4545 mL | 3.6362 mL | |
| 15 mM | 0.0970 mL | 0.4848 mL | 0.9696 mL | 2.4241 mL | |
| 20 mM | 0.0727 mL | 0.3636 mL | 0.7272 mL | 1.8181 mL | |
| 25 mM | 0.0582 mL | 0.2909 mL | 0.5818 mL | 1.4545 mL | |
| 30 mM | 0.0485 mL | 0.2424 mL | 0.4848 mL | 1.2121 mL | |
| 40 mM | 0.0364 mL | 0.1818 mL | 0.3636 mL | 0.9090 mL | |
| 50 mM | 0.0291 mL | 0.1454 mL | 0.2909 mL | 0.7272 mL | |
| 60 mM | 0.0242 mL | 0.1212 mL | 0.2424 mL | 0.6060 mL | |
| 80 mM | 0.0182 mL | 0.0909 mL | 0.1818 mL | 0.4545 mL | |
| 100 mM | 0.0145 mL | 0.0727 mL | 0.1454 mL | 0.3636 mL |
Tanimilast 関連分類
HY-19929 関連分類
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