Dynorphin A
Based on 2 publication(s) in Google Scholar
Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid 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 of neurological disease.
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- 純度 : 99.09%
- CAS 番号: 80448-90-4
- 分子式: C99H155N31O23
- 分子量:2147.48
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保管条件:
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)
MedChemExpress(MCE)の使用を引用している文献 Dynorphin A
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生物活性
製品説明
IC50 & Target
[3]|
Human Endogenous Metabolite |
Caspase 3 |
κ Opioid Receptor/KOR |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.41 nM
Compound: dynorphin A
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Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay
Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay
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[PMID: 25426797] |
| CHO | EC50 |
1.1 nM
Compound: 2, Dynorphin A
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Agonist activity at human kappa opioid receptor transfected in CHO cells by [35S]GTP-gamma-S binding assay
Agonist activity at human kappa opioid receptor transfected in CHO cells by [35S]GTP-gamma-S binding assay
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[PMID: 18487043] |
体外実験
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+]i and causes a significant loss of neurons[4].
dynorphin A (1 μM) inhibits the release of vasopressin (VP) from the isolated neural lobe[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse striatal neurons
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Concentration:10 μM
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Incubation Time:0, 24, 48, 72 h
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Result:Induced neuronal death (identified by the fragmentation and destruction of the cell body and neurites).
体内実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:24 h water-deprived male rats[5]
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Dosage:1 μg of 2 μL
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Administration:Intracerebroventricular injection
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Result:Inhibited vasopressin (VP) release 30 min upon injection.
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Animal Model:Male ddY mice[6]
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Dosage:15, 150, 1500 pmol/5 μL per day for 4 days
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Administration:Intracerebroventricular injection
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Result:Attenuated the repeated stress-induced escape failures from the shock.
化学情報
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CAS 番号 80448-90-4
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性状 Solid
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分子量 2147.48
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分子式 C99H155N31O23
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Color White to off-white
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別名
ダイノルフィンA
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配列
Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-Trp-Asp-Asn-Gln
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シーケンスの短縮
YGGFLRRIRPKLKWDNQ
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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)
Publications (2)
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Journal Impact Factor
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Most Recent
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Neuron
Astrocyte-mediated central amygdala microcircuit gates comorbid anxiety symptoms in chronic pain. [Abstract]2025 Oct 2:S0896-6273(25)00670-1. PMID: 41043420 -
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (46.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 100 mg/mL (46.57 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (1.40 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (1.40 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Zhang, et al.Dynorphin A as a Potential Endogenous Ligand for Four Members of the Opioid Receptor Gene Family. J Pharmacol Exp Ther. 1998 Jul;286(1):136-41. [Content Brief]
[2]. Aruna Sharma, et al. Monoclonal antibodies as novel neurotherapeutic agents in CNS injury and repair. Int Rev Neurobiol. 2012;102:23-45. [Content Brief]
[3]. I. N. SINGH, et al. Dynorphin A (1–17) induces apoptosis in striatal neurons in vitro through AMPA/kainate receptor-mediated cytochrome c release and caspase-3 activation. Neuroscience. 2003;122(4):1013-23. [Content Brief]
[4]. K F Hauser, et al. Dynorphin A (1-13) neurotoxicity in vitro: opioid and non-opioid mechanisms in mouse spinal cord neurons. Exp Neurol. 1999 Dec;160(2):361-75. [Content Brief]
[5]. B J Van de Heijning, et al. Dynorphin-A and vasopressin release in the rat: a structure-activity study. Neuropeptides. 1994 Jun;26(6):371-8. [Content Brief]
[6]. Takayoshi Mamiya, et al. Dynorphin a (1-13) alleviated stress-induced behavioral impairments in mice. Biol Pharm Bull. 2014;37(8):1269-73. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 0.4657 mL | 2.3283 mL | 4.6566 mL | 11.6416 mL |
| 5 mM | 0.0931 mL | 0.4657 mL | 0.9313 mL | 2.3283 mL | |
| 10 mM | 0.0466 mL | 0.2328 mL | 0.4657 mL | 1.1642 mL | |
| 15 mM | 0.0310 mL | 0.1552 mL | 0.3104 mL | 0.7761 mL | |
| 20 mM | 0.0233 mL | 0.1164 mL | 0.2328 mL | 0.5821 mL | |
| 25 mM | 0.0186 mL | 0.0931 mL | 0.1863 mL | 0.4657 mL | |
| 30 mM | 0.0155 mL | 0.0776 mL | 0.1552 mL | 0.3881 mL | |
| 40 mM | 0.0116 mL | 0.0582 mL | 0.1164 mL | 0.2910 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.