A 412997 dihydrochloride |
カタログ番号GC14610 |
選択的D4アゴニスト
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1347744-96-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
412997ジヒドロクロライドは、人間およびラットのD4受容体に対するKi値がそれぞれ7.9nMおよび12.1nMである、ドーパミンD4受容体の選択的アゴニストです[1]。
ドーパミンD4受容体はGタンパク質共役受容体であり、ドーパミンによって活性化されます。認知機能、パーキンソン病、中毒性行動などに重要な役割を果たしています。
412997ジヒドロクロライドは、選択的なドーパミンD4受容体アゴニストです。カルシウムフラックス機能アッセイでは、A-412997はラットのドーパミンD4受容体をEC50値28.4nMおよび固有活性0.83で活性化しました[1]。
Spontaneous Hypertensive Rat pups(SHRの子ネズミ)では、A 412997は5回繰り返される取得モデルで獲得を有意に増加させました。短期社会的記憶では、A 412997は2回目の調査時間を有意に短くしました。Wistar ラットと Dawley ラットでは、A 412997(3 μM/kg, 10 μM/kg)は運動活性を増加させました[2]。ラットでは、A 412997は非急速眼球運動(NREM)睡眠時間を減少させ覚醒時間を増加させます。また、A 412997は急速眼球運動(REM)睡眠時間も減少させてその開始時刻を遅らせます[3]。
References:
[1]. Moreland RB, Patel M, Hsieh GC, et al. A-412997 is a selective dopamine D4 receptor agonist in rats. Pharmacol Biochem Behav, 2005, 82(1): 140-147.
[2]. Browman KE, Curzon P, Pan JB, et al. A-412997, a selective dopamine D4 agonist, improves cognitive performance in rats. Pharmacol Biochem Behav, 2005, 82(1): 148-155.
[3]. Nakazawa S, Nakamichi K, Imai H, et al. Effect of dopamine D4 receptor agonists on sleep architecture in rats. Prog Neuropsychopharmacol Biol Psychiatry, 2015, 63: 6-13.
Cas No. | 1347744-96-0 | SDF | |
Chemical Name | (Z)-2-(4-(pyridin-2-yl)piperidin-1-yl)-N-(m-tolyl)acetimidic acid dihydrochloride | ||
Canonical SMILES | CC1=CC(/N=C(O)/CN2CCC(C3=CC=CC=N3)CC2)=CC=C1.Cl.Cl | ||
Formula | C19H23N3O.2HCl | M.Wt | 382.33 |
溶解度 | <38.23mg/ml in Water; <19.12mg/ml in DMSO | Storage | Desiccate at RT |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6155 mL | 13.0777 mL | 26.1554 mL |
5 mM | 0.5231 mL | 2.6155 mL | 5.2311 mL |
10 mM | 0.2616 mL | 1.3078 mL | 2.6155 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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