GX-674
Based on 1 Customer Validation
GX-674 is a potent, state-dependent, isoform-selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC50 of 0.1 nM at -40 mV.
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- 純度: 98.45%
- CAS 番号: 1432913-36-4
- 分子式: C21H13ClF2N6O3S2
- 分子量:534.95
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
製品説明
IC50 & Target
|
hNav1.7 0.1 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: 30
|
Inhibition of human NaV1.5 channel expressed in HEK293 cells by patch clamp electrophysiology assay
Inhibition of human NaV1.5 channel expressed in HEK293 cells by patch clamp electrophysiology assay
|
[PMID: 25927480] |
| HEK293 | IC50 |
30 nM
Compound: 30
|
Inhibition of human NaV1.7 channel expressed in HEK293 cells by patch clamp electrophysiology assay
Inhibition of human NaV1.7 channel expressed in HEK293 cells by patch clamp electrophysiology assay
|
[PMID: 25927480] |
| HEK293 | IC50 |
>10000 nM
Compound: 16
|
Inhibition of full length human Nav1.5 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.5 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
|
[PMID: 26985315] |
| HEK293 | IC50 |
0.2 nM
Compound: 16
|
Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
|
[PMID: 26985315] |
| HEK293 | IC50 |
0.3 nM
Compound: 16
|
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
|
[PMID: 26985315] |
| HEK293 | IC50 |
0.3 nM
Compound: 16
|
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at -150 mV by manual voltage clamp analysis
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at -150 mV by manual voltage clamp analysis
|
[PMID: 26985315] |
| HEK293 | IC50 |
0.8 nM
Compound: 16
|
Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
|
[PMID: 26985315] |
| HEK293 | IC50 |
3850 nM
Compound: 16
|
Inhibition of full length human Nav1.8 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at holding potential -20 mV by manual voltage clamp analysis
Inhibition of full length human Nav1.8 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at holding potential -20 mV by manual voltage clamp analysis
|
[PMID: 26985315] |
| HEK293 | IC50 |
6380 nM
Compound: 16
|
Inhibition of full length human Nav1.1 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -40 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.1 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -40 mV by automated voltage clamp analysis
|
[PMID: 26985315] |
| HEK293 | IC50 |
9330 nM
Compound: 16
|
Inhibition of full length human Nav1.3 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -50 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.3 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -50 mV by automated voltage clamp analysis
|
[PMID: 26985315] |
| HEK293 | IC50 |
>10000 nM
Compound: 16
|
Inhibition of full length human Nav1.4 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 by automated voltage clamp analysis
Inhibition of full length human Nav1.4 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 by automated voltage clamp analysis
|
[PMID: 26985315] |
化学情報
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CAS 番号 1432913-36-4
-
性状 Solid
-
分子量 534.95
-
分子式 C21H13ClF2N6O3S2
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Color Off-white to light brown
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SMILES
O=S(C1=CC(F)=C(OC2=CC=C(Cl)C=C2C3=CC=C4N=C(N)NC4=C3)C=C1F)(NC5=NC=NS5)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (93.47 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 (275 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
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 | 1.8693 mL | 9.3467 mL | 18.6933 mL | 46.7333 mL |
| 5 mM | 0.3739 mL | 1.8693 mL | 3.7387 mL | 9.3467 mL | |
| 10 mM | 0.1869 mL | 0.9347 mL | 1.8693 mL | 4.6733 mL | |
| 15 mM | 0.1246 mL | 0.6231 mL | 1.2462 mL | 3.1156 mL | |
| 20 mM | 0.0935 mL | 0.4673 mL | 0.9347 mL | 2.3367 mL | |
| 25 mM | 0.0748 mL | 0.3739 mL | 0.7477 mL | 1.8693 mL | |
| 30 mM | 0.0623 mL | 0.3116 mL | 0.6231 mL | 1.5578 mL | |
| 40 mM | 0.0467 mL | 0.2337 mL | 0.4673 mL | 1.1683 mL | |
| 50 mM | 0.0374 mL | 0.1869 mL | 0.3739 mL | 0.9347 mL | |
| 60 mM | 0.0312 mL | 0.1558 mL | 0.3116 mL | 0.7789 mL | |
| 80 mM | 0.0234 mL | 0.1168 mL | 0.2337 mL | 0.5842 mL |