SSD114 hydrochloride
目录号 : KM8484 CAS No. : 2319790-02-6 纯度 : 98%

SSD114 hydrochloride 是一种新型 GABAB 受体正变构调节剂。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.

体外研究

In the presence of 10 µM GABA, SSD114 hydrochloride at 25 µM significantly increases (to approximately 170% above basal levels) the [S]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 .

体内研究

The onset of loss of righting reflex (LORR) is reduced by pretreatment with SSD114 hydrochloride [F(5,30)=4.55, P<0.005]. Post 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, P<0.005]. Post 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.

分子式
C18H21ClF3N3O
分子量
387.83
CAS号
2319790-02-6
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 130 mg/mL (335.20 mM; Need ultrasonic)

H2O : 2 mg/mL (5.16 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 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
*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.25 mg/mL (8.38 mM); Clear solution

    此方案可获得 ≥ 3.25 mg/mL (8.38 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 3.25 mg/mL (8.38 mM); Suspended solution; Need ultrasonic

    此方案可获得 3.25 mg/mL (8.38 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 3.25 mg/mL (8.38 mM); Clear solution

    此方案可获得 ≥ 3.25 mg/mL (8.38 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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