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.
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: 99.07%
- CAS 番号: 1221349-53-6
- 分子式: C23H19F6N3O
- 分子量:467.41
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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
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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
生物活性
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.
化学情報
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CAS 番号 1221349-53-6
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性状 Solid
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分子量 467.41
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分子式 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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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
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.
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 (274 KB)
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SDS (254 KB)
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- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-110199 関連分類
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