Rotundine
Based on 1 publication(s) in Google Scholar
Rotundine is an antagonist of dopamine D1, D2 and D3 receptors with IC50s of 166 nM, 1.4 μM and 3.3 μM, respectively. Rotundine is also an antagonist of 5-HT1A with an IC50 of 370 nM.
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: 99.96%
- CAS 番号: 483-14-7
- 分子式: C21H25NO4
- 分子量:355.43
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 Rotundine
More5-HT Receptor アイソフォーム固有の製品をすべて表示
MoreDopamine Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
|
5-HT1A Receptor |
D1 Receptor 166 nM (IC50) |
D2 Receptor 1400 nM (IC50) |
D3 Receptor 3300 nM (IC50) |
5-HT1A Receptor 370 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
22.78 nM
Compound: 1
|
Inhibition of tissue factor procoagulant activity in LPS-stimulated human THP1 cells preincubated for 1 hr before LPS addition measured after 5 hrs
Inhibition of tissue factor procoagulant activity in LPS-stimulated human THP1 cells preincubated for 1 hr before LPS addition measured after 5 hrs
|
[PMID: 23199480] |
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
-
CAS 番号 483-14-7
-
性状 Solid
-
分子量 355.43
-
分子式 C21H25NO4
-
Color White to off-white
-
SMILES
COC1=CC=C2C(CN3CCC4=CC(OC)=C(OC)C=C4[C@]3([H])C2)=C1OC
-
別名
(-)-Tetrahydropalmatine; L-Tetrahydropalmatine
-
Structure Classification
-
Initial Source
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
-
Journal Impact Factor
-
Most Recent
溶剤 & 溶解度
DMF : 100 mg/mL (281.35 mM; Need ultrasonic)
DMSO : ≥ 100 mg/mL (281.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
Kunming mice, initially weighing 18 to 22 g are used in this study. Four groups of mice are given Rotundine (l-THP) (6.25, 12.5, and 18.75 mg/kg) or saline, respectively, once per day for 7 consecutive days, followed by a 5 d withdrawal period. On d 13, all animals are challenged with saline. On day 1, 7, and 13, after 40-min treatment with Rotundine or saline, the mice are put into the test boxes and locomotor activity is monitored for 60 min[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
-
データシート (275 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Wang JB, et al. l-tetrahydropalamatine: a potential new medication for the treatment of cocaine addiction. Future Med Chem. 2012 Feb;4(2):177-86. [Content Brief]
[2]. Liu YL, et al. Effects of l-tetrahydropalmatine on locomotor sensitization to oxycodone in mice. Acta Pharmacol Sin. 2005 May;26(5):533-8. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMF / DMSO | 1 mM | 2.8135 mL | 14.0675 mL | 28.1349 mL | 70.3373 mL |
| 5 mM | 0.5627 mL | 2.8135 mL | 5.6270 mL | 14.0675 mL | |
| 10 mM | 0.2813 mL | 1.4067 mL | 2.8135 mL | 7.0337 mL | |
| 15 mM | 0.1876 mL | 0.9378 mL | 1.8757 mL | 4.6892 mL | |
| 20 mM | 0.1407 mL | 0.7034 mL | 1.4067 mL | 3.5169 mL | |
| 25 mM | 0.1125 mL | 0.5627 mL | 1.1254 mL | 2.8135 mL | |
| 30 mM | 0.0938 mL | 0.4689 mL | 0.9378 mL | 2.3446 mL | |
| 40 mM | 0.0703 mL | 0.3517 mL | 0.7034 mL | 1.7584 mL | |
| 50 mM | 0.0563 mL | 0.2813 mL | 0.5627 mL | 1.4067 mL | |
| 60 mM | 0.0469 mL | 0.2345 mL | 0.4689 mL | 1.1723 mL | |
| 80 mM | 0.0352 mL | 0.1758 mL | 0.3517 mL | 0.8792 mL | |
| 100 mM | 0.0281 mL | 0.1407 mL | 0.2813 mL | 0.7034 mL |