JNJ-26489112
Based on 1 Customer Validation
JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na+ channels and N-type Ca2+ channels, and is effective as a K+ channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC50=35 μM) and CA-I (18 μM).
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: 99.31%
- CAS 番号: 871824-55-4
- 分子式: C9H11ClN2O4S
- 分子量:278.71
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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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Calcium Channel アイソフォーム固有の製品をすべて表示
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
34 μM
Compound: 4, JNJ-26489112
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Inhibition of rat Cav2.2-mediated calcium flux expressed in HEK cells by FDSS assay
Inhibition of rat Cav2.2-mediated calcium flux expressed in HEK cells by FDSS assay
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[PMID: 24205976] |
| HEK293 | IC50 |
70 μM
Compound: 4, JNJ-26489112
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Inhibition of rat Cav2.2-mediated calcium flux expressed in HEK cells at 0.07 Hz by whole-cell patch-clamp assay
Inhibition of rat Cav2.2-mediated calcium flux expressed in HEK cells at 0.07 Hz by whole-cell patch-clamp assay
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[PMID: 24205976] |
JNJ-26489112 inhibits calcium influx in response to depolarization (fluorescence-based assay) with an IC50 of 34 μM. In a whole-cell, patch-clamp experiment with low-frequency stimulation (0.07 Hz), intended to measure N-type channel activity directly, JNJ-26489112 causes a concentration-dependent increase in inhibition, with an IC50 of 70 μM. JNJ-26489112 is a KCNQ2 channel opener, particularly at -50 mV[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In adult male rats, JNJ-26489112 (p.o; 10 mg/kg) treatment shows the Cmax, tmax, F, t1/2, and AUC (total exposure) values in plasma were 9090 ng/mL (33 μM), 53 min, 95%, 8.2 h, and 53,200 ng-h/mL. Linear, dose-related increases in exposure were observed at 10, 30, and 300 mg/kg. JNJ-26489112 (i.v.; 2 mg/kg) treatment shows the Vdss is 390 mL/kg and the CL is 96 mL/h-kg. In female beagle dogs, JNJ-26489112 (p.o; 10 mg/kg) treatment shows the Cmax, tmax, F, t1/2, and AUC values in plasma are 11,500 ng/mL (41 μM), 55 min, 83%, 20 h, and 212,000 ng-h/mL. . JNJ-26489112 (i.v.; 2 mg/kg) treatment shows the the Vdss and CL values are 630 mL/kg and 30 mL/h-kg, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 871824-55-4
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性状 Solid
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分子量 278.71
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分子式 C9H11ClN2O4S
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Color White to light yellow
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SMILES
O=S(N)(NC[C@@H]1OC2=CC=C(Cl)C=C2OC1)=O
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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 : 100 mg/mL (358.80 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.
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 (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 3.5880 mL | 17.9398 mL | 35.8796 mL | 89.6990 mL |
| 5 mM | 0.7176 mL | 3.5880 mL | 7.1759 mL | 17.9398 mL | |
| 10 mM | 0.3588 mL | 1.7940 mL | 3.5880 mL | 8.9699 mL | |
| 15 mM | 0.2392 mL | 1.1960 mL | 2.3920 mL | 5.9799 mL | |
| 20 mM | 0.1794 mL | 0.8970 mL | 1.7940 mL | 4.4849 mL | |
| 25 mM | 0.1435 mL | 0.7176 mL | 1.4352 mL | 3.5880 mL | |
| 30 mM | 0.1196 mL | 0.5980 mL | 1.1960 mL | 2.9900 mL | |
| 40 mM | 0.0897 mL | 0.4485 mL | 0.8970 mL | 2.2425 mL | |
| 50 mM | 0.0718 mL | 0.3588 mL | 0.7176 mL | 1.7940 mL | |
| 60 mM | 0.0598 mL | 0.2990 mL | 0.5980 mL | 1.4950 mL | |
| 80 mM | 0.0448 mL | 0.2242 mL | 0.4485 mL | 1.1212 mL | |
| 100 mM | 0.0359 mL | 0.1794 mL | 0.3588 mL | 0.8970 mL |
JNJ-26489112 関連分類
HY-12596 関連分類
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