SKF 38393 hydrochloride 是一种多巴胺 D1 受体 (dopamine D1 receptor) 的选择性激动剂,IC50值为 110 nM。
生物活性 | SKF 38393 hydrochloride is a selective agonist of thedopamine D1 receptor (D1DR)with anIC50of 110 nM[1]. |
IC50& Target | |
体外研究 (In Vitro) | SKF-38393 hydrochloride induces a similar change in cytomorphology and increases the levels of media cAMP[2]. SKF-38393 hydrochloride (10 μmol/L; 1 hour) induces increased threonine-phosphorylation of DA- and cAMP-regulated phosphoprotein of Mr 32 kD (DARPP-32) in cultured GC cells[2].
Western Blot Analysis[2].
Cell Line: | GC cells | Concentration: | 10 μmol/L | Incubation Time: | 1 hour | Result: | Induced increased threonine-phosphorylation of DA- and cAMP-regulated phosphoprotein of Mr 32 kD (DARPP-32) in cultured GC cells. |
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体内研究 (In Vivo) | SKF-38393 hydrochloride (10 mg/kg; i.p.) blocks the 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) -induced depletion of glutathione[3]. SKF-38393 hydrochloride attenuates MPTP-induced depletion of dopamine[3]. SKF-38393 hydrochloride enhances the activity of superoxide dismutase and hence mimics the action of Selegiline[3]. SKF-38393 hydrochloride enhances the frequency but not the amplitude of tetrodotoxin-resistant excitatory postsynaptic currents which argues for a presynaptic locus of D1 action[4].
Animal Model: | Balb/c mice ( 20-25 g)[3].
| Dosage: | 5 mg/kg, 10 mg/kg | Administration: | Intraperitoneal injection | Result: | Blocked the MPTP-induced depletion of glutathione and attenuated MPTP-induced depletion of dopamine. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : ≥ 34 mg/mL(116.53 mM) H2O : 10 mg/mL(34.27 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 3.4274 mL | 17.1368 mL | 34.2736 mL | 5 mM | 0.6855 mL | 3.4274 mL | 6.8547 mL | 10 mM | 0.3427 mL | 1.7137 mL | 3.4274 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (7.13 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.13 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。
*以上所有助溶剂都可在本网站选购。 |