Hemicholinium 3
Based on 1 Customer Validation
Hemicholinium 3 is a competitive inhibitor of the high affinity choline transporter (HACU) with a Ki value of 25 nM. Hemicholinium 3, a neuromuscular blocking agent which inhibits the synthesis and the release of acetylcholine (ACh). Hemicholinium 3 inhibits the Epibatidine-evoked contraction and [3H]acetylcholine release with IC50s of 897 nM and 693 nM, respectively.
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: 99.89%
- CAS 番号: 312-45-8
- 分子式: C24H34Br2N2O4
- 分子量:574.35
-
保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
Hemicholinium 3 (HC-3) inhibits the presynaptic nicotinic acetylcholine receptors of myenteric neurons. HC-3 inhibits nAChRs located on the terminal region of myenteric neurons of guinea-pig longitudinal muscle strip preparation[2].
Hemicholinium 3 (HC-3) inhibits[3H]choline uptake with the Ki value of 13.3 μM in NCI-H69 cells[3].
HC-3 (1 mM) significantly inhibits cell viability and increases caspase-3/7 activity in NCI-H69 cells[3].
Hemicholinium 3 (Hemicholinium-3) inhibits sodium dependent high affinity choline uptake (IC50=18 nM)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:The human small cell lung carcinoma cell line NCI-H69
-
Concentration:1 mM
-
Incubation Time:Added every day for 2 days.
-
Result:Markedly inhibited cell viability.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
-
CAS 番号 312-45-8
-
性状 Solid
-
分子量 574.35
-
分子式 C24H34Br2N2O4
-
Color White to off-white
-
SMILES
C[N+]1(C)CC(C2=CC=C(C3=CC=C(C4(O)C[N+](C)(C)CCO4)C=C3)C=C2)(O)OCC1.[Br-].[Br-]
-
別名
Hemicholinium (dibromide); ヘミコリニウム-3
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : 50 mg/mL (87.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 33.33 mg/mL (58.03 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 10 mg/mL (17.41 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
純度とドキュメンテーション
-
データシート (274 KB)
-
SDS (481 KB)
- English - EN (481 KB)
- Français - FR (481 KB)
- Deutsch - DE (481 KB)
- Norwegian - NO (481 KB)
- Español - ES (481 KB)
- Swedish - SV (481 KB)
- Italian - IT (481 KB)
- Korean - KR (481 KB)
- Portuguese - PT (481 KB)
-
取扱説明書 (2659 KB)
参考文献
[2]. Péter Mandl, et al. Inhibitory effect of hemicholinium-3 on presynaptic nicotinic acetylcholine receptors located on the terminal region of myenteric motoneurons. Neurochem Int. 2006 Sep;49(4):327-33. [Content Brief]
[3]. Masato Inazu, et al. Functional expression of choline transporter-like protein 1 (CTL1) in small cell lung carcinoma cells: a target molecule for lung cancer therapy. Pharmacol Res. 2013 Oct;76:119-31. [Content Brief]
[4]. T K Chatterjee, et al. Methylpiperidine analog of hemicholinium-3: a selective, high affinity non-competitive inhibitor of sodium dependent choline uptake system. Eur J Pharmacol. 1988 May 10;149(3):241-8. [Content Brief]
[5]. J J Hagan, et al. Hemicholinium-3 impairs spatial learning and the deficit is reversed by cholinomimetics. Psychopharmacology (Berl). 1989;98(3):347-56. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.7411 mL | 8.7055 mL | 17.4110 mL | 43.5275 mL |
| 5 mM | 0.3482 mL | 1.7411 mL | 3.4822 mL | 8.7055 mL | |
| 10 mM | 0.1741 mL | 0.8705 mL | 1.7411 mL | 4.3527 mL | |
| 15 mM | 0.1161 mL | 0.5804 mL | 1.1607 mL | 2.9018 mL | |
| 20 mM | 0.0871 mL | 0.4353 mL | 0.8705 mL | 2.1764 mL | |
| 25 mM | 0.0696 mL | 0.3482 mL | 0.6964 mL | 1.7411 mL | |
| 30 mM | 0.0580 mL | 0.2902 mL | 0.5804 mL | 1.4509 mL | |
| 40 mM | 0.0435 mL | 0.2176 mL | 0.4353 mL | 1.0882 mL | |
| 50 mM | 0.0348 mL | 0.1741 mL | 0.3482 mL | 0.8705 mL | |
| DMSO | 60 mM | 0.0290 mL | 0.1451 mL | 0.2902 mL | 0.7255 mL |
| 80 mM | 0.0218 mL | 0.1088 mL | 0.2176 mL | 0.5441 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.