Dynorphin A 是一种内源性阿片肽,参与中枢神经系统 (CNS) 的抑制性神经传递。Dynorphin A 是一种高效的 kappa 阿片受体 (KOR) 激动剂,也是其他阿片受体的激动剂,如 mu (MOR) 和 delta (DOR)。Dynorphin A 可诱导神经元死亡,可用于神经系统疾病的相关研究。
生物活性 | Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potentkappaopioid receptor(KOR)agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research ofneurological disease[1][2]. |
IC50& Target[3] | Human Endogenous Metabolite | Caspase 3 | κ Opioid Receptor/KOR |
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体外研究 (In Vitro) | Dynorphin A (10 μM, 4 h/72 h) increases caspase-3 activity and the level of cytochrome c released from mitochondria in mouse striatal neurons, and induces neuronal death[3]. dynorphin A (33 μM, 4 h) elevates [Ca2+]iand causes a significant loss of neurons[4]. dynorphin A (1 μM) inhibits the release of vasopressin (VP) from the isolated neural lobe[5].
Cell Viability Assay[3] Cell Line: | Mouse striatal neurons | Concentration: | 10 μM | Incubation Time: | 0, 24, 48, 72 h | Result: | Induced neuronal death (identified by the fragmentation and destruction of the cell body and neurites). |
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体内研究 (In Vivo) | Dynorphin A (intracerebroventricular injection, 1 μg of 2 μL, a single dose) inhibits vasopressin (VP) release in 24 h water-deprived male rats[5]. Dynorphin A (intracerebroventricular injection, 500 pmol/5 μL per day for 4 d) alleviates stress-induced behavioral impairments in ddY mice accompanied by regulation of the 5-HTergic system in the brain[6].
Animal Model: | 24 h water-deprived male rats[5] | Dosage: | 1 μg of 2 μL | Administration: | Intracerebroventricular injection | Result: | Inhibited vasopressin (VP) release 30 min upon injection. |
Animal Model: | Male ddY mice[6] | Dosage: | 15, 150, 1500 pmol/5 μL per day for 4 days | Administration: | Intracerebroventricular injection | Result: | Attenuated the repeated stress-induced escape failures from the shock. |
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Formula | |
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Sequence | Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-Trp-Asp-Asn-Gln |
Sequence Shortening | |
中文名称 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Sealed storage, away from moisture and light Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: DMSO : 120 mg/mL(55.88 mM;Need ultrasonic) 配制储备液 1 mM | 0.4657 mL | 2.3283 mL | 4.6566 mL | 5 mM | 0.0931 mL | 0.4657 mL | 0.9313 mL | 10 mM | 0.0466 mL | 0.2328 mL | 0.4657 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 and light)。-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 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 3 mg/mL (1.40 mM); Clear solution
此方案可获得 ≥ 3 mg/mL (1.40 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 30.0 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-CDin saline) Solubility: ≥ 3 mg/mL (1.40 mM); Clear solution
此方案可获得 ≥ 3 mg/mL (1.40 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 30.0 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。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 3 mg/mL (1.40 mM); Clear solution
此方案可获得 ≥ 3 mg/mL (1.40 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 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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