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.
For research use only. We do not sell to patients.
- Purity : 99.71%
- CAS No.: 1239278-59-1
- Formula: C30H30Cl2F2N2O8S
- Molecular Weight:687.54
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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] |
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1239278-59-1
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Appearance Solid
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Molecular Weight 687.54
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Formula 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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Synonyms
CHF-6001
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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
Solvent & Solubility
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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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Cotton Pellet Granuloma
Cotton pellet granuloma is a classical in vivo chronic inflammation model used to evaluate the anti-inflammatory potential of test substances by measuring their ability to inhibit granuloma tissue formation around an implanted foreign body (cotton pellet) in rodents. The method is based on the biological response to a sterile implanted material, which induces proliferative phase inflammation characterized by fibroblast proliferation and collagen-rich granuloma formation, and the final readout reflects the extent of chronic inflammatory tissue growth surrounding the pellet. In multiple preclinical pharmacological evaluations, inhibition of cotton pellet-induced granuloma formation has been used as an indicator of anti-inflammatory activity in both synthetic and natural product screening contexts.
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Carrageenan-Induced Paw Edema
Carrageenan-induced paw edema is an acute inflammation model in which intraplantar injection of carrageenan induces localized inflammatory swelling characterized by vascular permeability, leukocyte infiltration, and production of inflammatory mediators such as prostaglandins and cytokines, making it widely used to evaluate anti-inflammatory agents in vivo. The resulting paw volume or thickness increase is quantified over time as a direct readout of inflammatory intensity and drug efficacy, typically reflecting cyclooxygenase-mediated prostaglandin-driven edema formation and immune cell recruitment in peripheral tissue[20].
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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
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 Related Classifications
HY-19929 Related Classifications
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