Ro 10-5824 dihydrochloride
目录号 : GC12428
Ro 10-5824 dihydrochloride 是一种选择性多巴胺 D4 受体部分激动剂，Ki 为 5.2 nM。
Cas No.:189744-94-3
Sample solution is provided at 25 µL, 10mM.
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Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
RO-10-5824 shows high affinity binding with a Ki=5.2±0.9 nM (n=3), 250-fold selectivity vs human D3R, and >1000 fold selectivity for D4 vs human D2, D1, and D5 receptors. RO-10-5824 stimulates 35S-GTPγS binding with an EC50 value of 205±67 nM (n=7) and maximal induction at 36±4% above basal level[2].
Ro 10-5824 (3 mg/kg) increases the success rate in the ORD task. At doses of 1 and 3 mg/kg, Ro 10-5824 increases baseline gamma band activity in the frontal cortex. Ro 10-5824 has no effect on spontaneous locomotion[1]. RO-10-5824 (10.0 mg/kg) does not increase center entries in the open field in a single 60-min session without the novel object present, nor does it increase overall transitions in the initial experiment with C57 mice[2].
References:
[1]. Nakazawa S, et al. Behavioral and neurophysiological effects of Ro 10-5824, a dopamine D4 receptor partial agonist, in common marmosets. Psychopharmacology (Berl). 2015 Sep;232(17):3287-95.
[2]. Powell SB, et al. RO-10-5824 is a selective dopamine D4 receptor agonist that increases novel object exploration in C57 mice. Neuropharmacology. 2003 Mar;44(4):473-81.
Animal experiment: | In the experiment, 39 C57 and 40 DBA mice are tested over a three-day period. On days 1 and 2, mice are placed into the VT for 60 min and locomotor behavior is recorded. On the third day, mice are placed into the VT chamber for 60 min. Following the 60-min period, mice are removed from the chambers and administered 0, 1.0, 3.0, or 10.0 mg/kg of RO-10-5824 (n=9-11 per group). Mice are assigned to drug group pseudo-randomly, with each dose being represented in a cage of four mice. A novel paper cup measuring 9.5 cm in height and 7.5 cm in diameter at the rim is placed upside down in the center of each open field and secured to the floor with tape. Mice are returned to the VT 10 min following injection and tested for an additional 30 min. |
References: [1]. Nakazawa S, et al. Behavioral and neurophysiological effects of Ro 10-5824, a dopamine D4 receptor partial agonist, in common marmosets. Psychopharmacology (Berl). 2015 Sep;232(17):3287-95. | |
| Cas No. | 189744-94-3 | SDF | |
| 化学名 | 2-methyl-5-((4-phenyl-5,6-dihydropyridin-1(2H)-yl)methyl)pyrimidin-4(3H)-imine dihydrochloride | ||
| Canonical SMILES | CC(N1)=NC=C(C1=N)CN2CC=C(C3=CC=CC=C3)CC2.Cl.Cl | ||
| 分子式 | C17H20N4.2HCl | 分子量 | 353.29 |
| 溶解度 | H2O : 100 mg/mL (283.05 mM; Need ultrasonic); DMSO : 8.33 mg/mL (23.58 mM; Need ultrasonic) | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8305 mL | 14.1527 mL | 28.3054 mL |
| 5 mM | 0.5661 mL | 2.8305 mL | 5.6611 mL |
| 10 mM | 0.2831 mL | 1.4153 mL | 2.8305 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet