SSD114 hydrochloride
目录号 : GC34362
SSD114hydrochloride是一种新型GABAB受体正变构调节剂。
Cas No.:2319790-02-6
Sample solution is provided at 25 µL, 10mM.
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SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
In the presence of 10 µM GABA, SSD114 hydrochloride at 25 µM significantly increases (to approximately 170% above basal levels) the [35S]GTPγS stimulation induced by GABA alone. SSD114 hydrochloride, added at 15 and 30 µM, induces a leftward shift of the GABA concentration-response curve with a slight concomitant increase of maximal GABA stimulation at the highest concentration. In the presence of both 15 and 30 µM SSD114 hydrochloride, the EC50 for GABA decreases by 2 and 2.5 fold, respectively, while the maximal stimulation (Emax) is potentiated only at the concentration of 30 µM, reaching 161±5.09% over the basal value[1] .
The onset of loss of righting reflex (LORR) is reduced by pretreatment with SSD114 hydrochloride [F(5,30)=4.55, PPost hoc analysis indicates that the onset of LORR is significantly lower in mouse groups pretreated with doses of SSD114 hydrochloride equal to or higher than 10 mg/kg than in vehicle-treated mice. The duration of LORR is increased by pretreatment with SSD114 hydrochloride [F(5,30)=4.81, PPost hoc analysis indicates that the duration of LORR is significantly longer in mouse groups pretreated with 10 and 100 mg/kg SSD114 hydrochloride than in vehicle-treated mice[1].
[1]. Porcu A, et al. In vitro and in vivo pharmacological characterization of SSD114, a novel GABAB positive allosteric modulator. Eur J Pharmacol. 2016 Nov 15;791:115-123.
Cell experiment: | Cells are transfected and seeded into 96-well microplates. 24 h after transfection, cells are washed twice with PBS and incubated in the presence or absence of SSD114 hydrochloride (different concentrations) for 15 min before substrate addition in a 96-well microplate. The Bioluminescence resonance energy transfer (BRET) ratio is calculated as the emission of YFP (530 to 570 nm) over the emission of RLuc (370 to 470 nm). The curves are fitted using Graph Pad Prism 5.0. The amplitude-weighted mean time constant is obtained by fitting the BRET recovery phase to a double exponential function. ΔBRET is calculated as the difference between the basal and the plateau of the BRET signal[1]. |
Animal experiment: | Male Sprague-Dawley rats and DBA mice, weighing 200 to 250 and 20 to 25 g, respectively, are used. On the test day, mice are divided into six groups (n=6 each) matched by body weight. Mice are treated acutely and intraperitoneally with 0, 1, 3, 10, 30, and 100 mg/kg SSD114 hydrochloride and sedation/hypnosis is measured. Specifically, after baclofen injection, each mouse is placed on its back once every 60 s until it is unable to right itself within 60 s. The time between baclofen injection and the start of the 60-s interval during which the mouse is unable to right itself is measured as the onset of loss of righting reflex (LORR). Each mouse is then left undisturbed on its back until it spontaneously regained its righting reflex (determined as having at least three paws under its body). Complete recovery of the righting reflex is defined as the mouse being able to turn itself upright twice more within 60 s. If this criterion is not fulfilled, the mouse is left undisturbed until it spontaneously regained its righting reflex. The time between loss and recovery of righting reflex is monitored in each mouse and defined as the duration of LORR. Observations are conducted by an operator unaware of the drug treatment[1]. |
References: [1]. Porcu A, et al. In vitro and in vivo pharmacological characterization of SSD114, a novel GABAB positive allosteric modulator. Eur J Pharmacol. 2016 Nov 15;791:115-123. | |
| Cas No. | 2319790-02-6 | SDF | |
| Canonical SMILES | FC(C1=CC=C(C2=CC(OC)=NC(NC3CCCCC3)=N2)C=C1)(F)F.[H]Cl | ||
| 分子式 | C18H21ClF3N3O | 分子量 | 387.83 |
| 溶解度 | DMSO : 130 mg/mL (335.20 mM; Need ultrasonic); H2O : 2 mg/mL (5.16 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | Store at -20°C |
| 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 | 2.5784 mL | 12.8922 mL | 25.7845 mL |
| 5 mM | 0.5157 mL | 2.5784 mL | 5.1569 mL |
| 10 mM | 0.2578 mL | 1.2892 mL | 2.5784 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。
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet