TC-I 2014
Based on 1 Customer Validation
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.07%
- CAS. Nr.: 1221349-53-6
- Formel: C23H19F6N3O
- Molecular Weight:467.41
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Neuronal Signaling Compound Library
HY-L013
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Mechanoreceptors Compound Library
HY-L095
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Pain-Related Compound Library
HY-L139
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Ion Channel Compound Library
HY-L166
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biologische Aktivität
TRPM8[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.413 nM
Compound: 5
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Inhibition of human TRPM8 expressed in HEK293 cells assessed as inhibition of cold-induced channel current by whole cell electrophysiology
Inhibition of human TRPM8 expressed in HEK293 cells assessed as inhibition of cold-induced channel current by whole cell electrophysiology
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[PMID: 21128593] |
| HEK293 | IC50 |
0.8 nM
Compound: 5
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Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay
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[PMID: 21128593] |
| HEK293 | IC50 |
3 nM
Compound: 5
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Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay
Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay
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[PMID: 21128593] |
| HEK293 | IC50 |
4 nM
Compound: 5
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Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay
Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay
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[PMID: 21128593] |
TC-I 2014 (compound 5) potently inhibits cold-induced TRPM8 currents in HEK293 cells stably expressing canine or human TRPM8, with IC50 values of 0.413 and 1 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS[1].
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Dosage:3, 5.6, 10 mg/kg.
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Administration:Orally once.
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Result:Produced greater than 90% inhibition at 3, 5.6, and 10 mg/kg administered 2 h prior to icilin challenge.
Chemical Information
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CAS. Nr. 1221349-53-6
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Appearance Solid
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Molecular Weight 467.41
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Formel C23H19F6N3O
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Color White to off-white
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SMILES
FC(C1=CC=CC=C1C2=CC(C(F)(F)F)=C3C(N=C(C4=NOC5(CCCCC5)C4)N3)=C2)(F)F
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 250 mg/mL (534.86 mM; Need ultrasonic; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 2.1394 mL | 10.6972 mL | 21.3945 mL | 53.4862 mL |
| 5 mM | 0.4279 mL | 2.1394 mL | 4.2789 mL | 10.6972 mL | |
| 10 mM | 0.2139 mL | 1.0697 mL | 2.1394 mL | 5.3486 mL | |
| 15 mM | 0.1426 mL | 0.7131 mL | 1.4263 mL | 3.5657 mL | |
| 20 mM | 0.1070 mL | 0.5349 mL | 1.0697 mL | 2.6743 mL | |
| 25 mM | 0.0856 mL | 0.4279 mL | 0.8558 mL | 2.1394 mL | |
| 30 mM | 0.0713 mL | 0.3566 mL | 0.7131 mL | 1.7829 mL | |
| 40 mM | 0.0535 mL | 0.2674 mL | 0.5349 mL | 1.3372 mL | |
| 50 mM | 0.0428 mL | 0.2139 mL | 0.4279 mL | 1.0697 mL | |
| 60 mM | 0.0357 mL | 0.1783 mL | 0.3566 mL | 0.8914 mL | |
| 80 mM | 0.0267 mL | 0.1337 mL | 0.2674 mL | 0.6686 mL | |
| 100 mM | 0.0214 mL | 0.1070 mL | 0.2139 mL | 0.5349 mL |
TC-I 2014 Related Classifications
HY-110199 Related Classifications
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