SKF38393 HCl|62717-42-4|((±)-SKF-38393 hydrochloride; SKF-38393A)-陌孚医药/Medlife

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SKF38393 HCl (Synonyms: (±)-SKF-38393 hydrochloride; SKF-38393A)

目录号: PC14382 纯度: ≥98%

CAS No. :62717-42-4

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中文名称	SKF38393 HCl
中文别名	2,3,4,5-四氢-1-苯基-1H-3-苯并氮杂卓-7,8-二醇盐酸盐
英文名称	SKF38393 HCl
英文别名	1-Phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol hydrochloride;(+/-)-SKF-38393 hydrochloride;(±)-SKF38393HYDROCHLORIDE;1H-3-Benzazepine-7,8-diol,2,3,4,5-tetrahydro-1-phenyl-, hydrochloride (1:1);2-phenyl-4-azabicyclo[5.4.0]undeca-7,9,11-triene-9,10-diol;5-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol,hydrochloride;SKF 38393 Hydrochloride;(±)-SKF-38393 hydrochloride;1H-3-Benzazepine-7,8-diol,2,3,4,5-tetrahydro-1-phenyl-,hydrochloride;SKF-38393A;SKF 38393A;SKF38393 HCl;SKF 38393 (hydrochloride);1H-3-Benzazepine-7,8-diol, 2,3,4,5-tetrahydro-1-phenyl-, hydrochloride;1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol hydrochloride;skf38393-hcl;MLS000859931;SKF 38393 HCl;(y)-SKF-
Cas No.	62717-42-4
分子式	C₁₆H₁₈ClNO₂
分子量	291.77
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

SKF 38393 hydrochloride is a selective agonist of the dopamine D1 receptor (D1DR) with an IC₅₀ of 110 nM.

性状

Solid

IC50 & Target[1][2]

IC50: 110 nM (D1DR)

体外研究(In Vitro)

SKF-38393 hydrochloride induces a similar change in cytomorphology and increases the levels of media cAMP.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis.

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.

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.
SKF-38393 hydrochloride attenuates MPTP-induced depletion of dopamine.
SKF-38393 hydrochloride enhances the activity of superoxide dismutase and hence mimics the action of Selegiline.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Balb/c mice ( 20-25 g).
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.

运输条件

Room temperature or refrigerated transportation.

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)

参考文献

[1]. Altar CA, et al. Picomolar affinity of 125I-SCH 23982 for D1 receptors in brain demonstrated with digital subtraction auto radiography. J Neurosci. 1987 Jan;7(1):213-222. [Information]

[2]. Mayerhofer A, et al. Functional Dopamine-1 Receptors and DARPP-32 Are Expressed in Human Ovary and Granulosa Luteal Cells 体外研究. J Clin Endocrinol Metab. 1999 Jan;84(1):257-64. [Information]

[3]. Muralikrishnan D, et al. SKF-38393, a dopamine receptor agonist, attenuates 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced neurotoxicity. Brain Res. 2001 Feb 23;892(2):241-7. [Information]

[4]. Bouron A, et al. The D1 dopamine receptor agonist SKF-38393 stimulates the release of glutamate in the hippocampus. Neuroscience. 1999;94(4):1063-70. [Information]

溶解度数据

体外研究:

DMSO : ≥ 34 mg/mL (116.53 mM)

H₂O : 10 mg/mL (34.27 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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 (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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