A 412997 dihydrochloride
目录号 : GC14610
Selective D4 agonist
Cas No.:1347744-96-0
Sample solution is provided at 25 µL, 10mM.
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A 412997 dihydrochloride is a selective agonist of dopamine D4 receptor with Ki values of 7.9 and 12.1 nM for human and rat D4 receptors, respectively [1].
Dopamine D4 receptor is a G protein-coupled receptor and is activated by dopamine. It plays an important role in cognition, Parkinsons disease, addictive behaviors and so on.
A 412997 dihydrochloride is a selective dopamine D4 receptor agonist. In calcium flux functional assays, A-412997 activated the rat dopamine D4 receptor with EC50 value and intrinsic activity of 28.4 nM and 0.83, respectively [1].
In Spontaneous Hypertensive Rat pups (SHR pups), A 412997 significantly increased acquisition in the 5-trial repeated acquisition model. In the short-term social memory, A 412997 significantly shortened the second investigation time. In Wistar rats and Dawley rats, A 412997 (3 μM/kg, 10 μM/kg) increased locomotor activity [2]. In rats, A 412997 reduced non-rapid eye movement (NREM) sleep duration and increased waking duration. Also, A 412997 reduced rapid eye movement (REM) sleep duration and delayed the onset of REM sleep [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 | |
| 化学名 | (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 | ||
| 分子式 | C19H23N3O.2HCl | 分子量 | 382.33 |
| 溶解度 | <38.23mg/ml in Water; <19.12mg/ml in DMSO | 储存条件 | Desiccate at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet