TC-N 1752
Based on 1 Customer Validation
TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain.
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: 99.67%
- CAS 番号: 1211866-85-1
- 分子式: C25H27F3N6O3
- 分子量:516.52
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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
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hNav1.7 0.17 μM (IC50) |
hNav1.8 0.1 μM (IC50) |
hNav1.3 0.3 μM (IC50) |
hNav1.4 0.4 μM (IC50) |
hNav1.5 1.1 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: 52
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Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.3 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.3 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
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[PMID: 21634377] |
| HEK293 | IC50 |
>10 μM
Compound: 52
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Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.4 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.4 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
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[PMID: 21634377] |
| HEK293 | IC50 |
>10 μM
Compound: 52
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Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.5 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.5 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
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[PMID: 21634377] |
| HEK293 | IC50 |
>10 μM
Compound: 52
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Inhibition of human Erg expressed in human HEK293 cells by patch-clamp electrophysiological assay
Inhibition of human Erg expressed in human HEK293 cells by patch-clamp electrophysiological assay
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[PMID: 21634377] |
| HEK293 | IC50 |
0.3 μM
Compound: 52
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Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.3 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.3 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
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[PMID: 21634377] |
| HEK293 | IC50 |
0.4 μM
Compound: 52
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Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.4 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.4 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
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[PMID: 21634377] |
| HEK293 | IC50 |
0.5 μM
Compound: 52
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Inhibition of human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay
Inhibition of human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay
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[PMID: 21634377] |
| HEK293 | IC50 |
1.1 μM
Compound: 52
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Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.5 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.5 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
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[PMID: 21634377] |
| HEK293 | IC50 |
170 nM
Compound: 52
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Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay
Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay
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[PMID: 21634377] |
| HEK293 | IC50 |
2.2 μM
Compound: 52
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Inhibition of 20% inactivated TTX-resistant rat sodium channel Nav1.8 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
Inhibition of 20% inactivated TTX-resistant rat sodium channel Nav1.8 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay
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[PMID: 21634377] |
| HEK293 | IC50 |
3.3 μM
Compound: 52
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Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay in presence of 5% human serum albumin
Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay in presence of 5% human serum albumin
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[PMID: 21634377] |
| HEK293 | IC50 |
3.6 μM
Compound: 52
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Inhibition of fully inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay
Inhibition of fully inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay
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[PMID: 21634377] |
| HEK293 | IC50 |
5.2 μM
Compound: 52
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Inhibition of human cardiac sodium channel Nav1.5 expressed in human HEK293 cells by patch-clamp electrophysiological assay
Inhibition of human cardiac sodium channel Nav1.5 expressed in human HEK293 cells by patch-clamp electrophysiological assay
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[PMID: 21634377] |
体外実験
TC-N 1752 (compound 52) state-dependently inhibits Nav1.7, with IC50 of 170 nM on channels that are 20% inactivated and IC50 of 3.6 μM on fully noninactivated channels[1].
TC-N 1752 inhibits hNav1.7, hNav1.8, hNav1.9, rNav1.9, and mNav1.9 with IC50s of 0.2, 0.1, 1.6, 0.5 and 1.4 μM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
TC-N 1752 (3-30 mg/kg; p.o.) decreases thermal hyperalgesia produced by inflammation[3].
TC-N 1752 (5 mg/mL; 500 μL; i.v.) attenuates complete Freund’s adjuvant (CFA)-induced sensitization of C-fiber nociceptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats were injected intraplantar with Formalin[1]
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Dosage:3, 10, 20, 30 mg/kg
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Administration:Administered p.o. 120 min prior to Formalin
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Result:Showed analgesic efficacy starting at the dose of 3 mg/kg, with full efficacy at 20 mg/kg dose.
化学情報
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CAS 番号 1211866-85-1
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性状 Solid
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分子量 516.52
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分子式 C25H27F3N6O3
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Color White to off-white
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SMILES
FC(F)(F)OC(C=C1)=CC=C1COC(CC2)CCN2C3=NC=NC(NC4=C(C(NC(C)=O)=CC=C4)C)=N3
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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 : 125 mg/mL (242.00 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 (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Bregman H, et, al. Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain. J Med Chem. 2011 Jul 14;54(13):4427-45. [Content Brief]
[2]. Lin Z, et, al. Biophysical and Pharmacological Characterization of Nav1.9 Voltage Dependent Sodium Channels Stably Expressed in HEK-293 Cells. PLoS One. 2016 Aug 24;11(8):e0161450. [Content Brief]
[3]. Matson DJ, et, al. Inhibition of Inactive States of Tetrodotoxin-Sensitive Sodium Channels Reduces Spontaneous Firing of C-Fiber Nociceptors and Produces Analgesia in Formalin and Complete Freund's Adjuvant Models of Pain. PLoS One. 2015 Sep 17;10(9):e013 [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 | 1.9360 mL | 9.6802 mL | 19.3603 mL | 48.4008 mL |
| 5 mM | 0.3872 mL | 1.9360 mL | 3.8721 mL | 9.6802 mL | |
| 10 mM | 0.1936 mL | 0.9680 mL | 1.9360 mL | 4.8401 mL | |
| 15 mM | 0.1291 mL | 0.6453 mL | 1.2907 mL | 3.2267 mL | |
| 20 mM | 0.0968 mL | 0.4840 mL | 0.9680 mL | 2.4200 mL | |
| 25 mM | 0.0774 mL | 0.3872 mL | 0.7744 mL | 1.9360 mL | |
| 30 mM | 0.0645 mL | 0.3227 mL | 0.6453 mL | 1.6134 mL | |
| 40 mM | 0.0484 mL | 0.2420 mL | 0.4840 mL | 1.2100 mL | |
| 50 mM | 0.0387 mL | 0.1936 mL | 0.3872 mL | 0.9680 mL | |
| 60 mM | 0.0323 mL | 0.1613 mL | 0.3227 mL | 0.8067 mL | |
| 80 mM | 0.0242 mL | 0.1210 mL | 0.2420 mL | 0.6050 mL | |
| 100 mM | 0.0194 mL | 0.0968 mL | 0.1936 mL | 0.4840 mL |
TC-N 1752 関連分類
HY-107405 関連分類
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