Dynorphin A (trifluoroacetate salt)
(Synonyms: Dynorphin A (1-17)) 目录号 : GC52500Dynorphin A (trifluoroacetate salt)是一种内源性阿片肽，可激活孤儿受体XOR1-K+通道，EC50值为45nM。
Sample solution is provided at 25 µL, 10mM.
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Dynorphin A (trifluoroacetate salt) is an endogenous opioid peptide that activates orphan receptor XOR1-K+ channel, with an EC50 value of 45nM [1]. Dynorphin A (trifluoroacetate salt) can bind to and activate all members of the opioid receptor family, regulating the membrane conductance of neurons[2]. Dynorphin A (trifluoroacetate salt) has been widely used in studies related to drug dependence and addiction, as well as in the regulation of neural functions[3].
In vitro, Dynorphin A (trifluoroacetate salt) treatment at 10μM for 4 hours significantly induced caspase-3 activation in the mouse striatal neuronal cells, and increased the level of cytochrome c released from mitochondria[4]. Treatment with Dynorphin A (trifluoroacetate salt) (10μM) for 16 hours can induce a strong migration response activity in HEK293 cells that express Mac-1[5]. Treatment with 100μM Dynorphin A (trifluoroacetate salt) for 96 hours significantly induced the death of mouse spinal cord neurons [6]. Treatment with 10μM Dynorphin A (trifluoroacetate salt) for 48 hours significantly reduced the viability of U2OS cells, causing mitochondrial dysfunction and down-regulating key mitochondrial regulatory factors, including PGC-1α, Nrf1 and TFAM[7]. Treatment with 1μM Dynorphin A (trifluoroacetate salt) for 1 hour significantly inhibited the nuclear translocation of NF-κB/p65 in THP-1 cells stimulated by lipopolysaccharide (LPS) [8].
References:
[1] Zhang S, Yu L. Identification of dynorphins as endogenous ligands for an opioid receptor-like orphan receptor[J]. Journal of Biological Chemistry, 1995, 270(39): 22772-22776.
[2] Zhang S, Tong Y, Tian M, et al. Dynorphin A (trifluoroacetate salt) as a potential endogenous ligand for four members of the opioid receptor gene family[J]. The Journal of pharmacology and experimental therapeutics, 1998, 286(1): 136-141.
[3] Shippenberg T S, Zapata A, Chefer V I. Dynorphin A (trifluoroacetate salt)nd the pathophysiology of drug addiction[J]. Pharmacology & therapeutics, 2007, 116(2): 306-321.
[4] Singh I N, Goody R J, Goebel S M, et al. Dynorphin A (trifluoroacetate salt) (1–17) induces apoptosis in striatal neurons in vitro through AMPA/kainate receptor-mediated cytochrome c release and caspase-3 activation[J]. Neuroscience, 2003, 122(4): 1013.
[5] Podolnikova N P, Brothwell J A, Ugarova T P. The opioid peptide Dynorphin A (trifluoroacetate salt) induces leukocyte responses via integrin Mac-1 (αMβ2, CD11b/CD18)[J]. Molecular pain, 2015, 11: s12990-015-0027-0.
[6] Hauser K F, Knapp P E, Turbek C S. Structure–activity analysis of Dynorphin A (trifluoroacetate salt) toxicity in spinal cord neurons: intrinsic neurotoxicity of Dynorphin A (trifluoroacetate salt) and its carboxyl-terminal, nonopioid metabolites[J]. Experimental neurology, 2001, 168(1): 78-87.
[7] Dai Y, Zhang J, Peng Y, et al. Dynorphin A (trifluoroacetate salt) Impairs Mitochondrial Biogenesis in Osteosarcoma Cells by Increasing SP‐1[J]. Journal of Biochemical and Molecular Toxicology, 2025, 39(9): e70451.
[8] Fazalul Rahiman S S, Morgan M, Gray P, et al. Dynorphin 1-17 and its N-terminal biotransformation fragments modulate lipopolysaccharide-stimulated nuclear factor-kappa B nuclear translocation, interleukin-1beta and tumor necrosis factor-alpha in differentiated THP-1 cells[J]. PLoS One, 2016, 11(4): e0153005.
Dynorphin A (trifluoroacetate salt)是一种内源性阿片肽，可激活孤儿受体XOR1-K+通道，EC50值为45nM[1]。Dynorphin A (trifluoroacetate salt)能结合并激活所有阿片受体家族成员，调节神经元膜电导[2]。Dynorphin A (trifluoroacetate salt)已广泛应用于药物依赖与成瘾相关研究及神经功能调控领域[3]。
在体外，使用10μM的Dynorphin A (trifluoroacetate salt)处理小鼠纹状体神经元细胞4小时，可显著诱导caspase-3活化并增加线粒体细胞色素c的释放[4]。用10μM的Dynorphin A (trifluoroacetate salt)处理表达Mac-1的HEK293细胞16小时，能诱导强烈的细胞迁移反应[5]。以100μM的Dynorphin A (trifluoroacetate salt)处理小鼠脊髓神经元96小时，可显著诱导神经元死亡[6]。用10μM的Dynorphin A (trifluoroacetate salt)处理U2OS细胞48小时，能显著降低细胞活力，引起线粒体功能障碍并下调PGC-1α、Nrf1和TFAM关键线粒体调控因子[7]。以1μM的Dynorphin A (trifluoroacetate salt)处理THP-1细胞1小时，可显著抑制脂多糖(LPS)刺激诱导的NF-κB/p65核转位[8]。
| Cell experiment [1]: | |
Cell lines | U2OS cells |
Preparation Method | U2OS cells were cultured in DMEM medium, which was supplemented with 10% fetal bovine serum (FBS), L-glutamine and 1% penicillin/streptomycin. The cells were cultured under conditions of 37°C and 5% CO2. 3000 U2OS cells were inoculated into each well of a 96-well plate. The cells were treated with Dynorphin A (trifluoroacetate salt) at concentrations of 0.1, 0.5, 1, 5, 10, 50 and 100μM for 48 hours. 10μl of CCK-8 reagent was added to each well and incubated for 2 hours. Then, the absorbance value was measured at 450nm. |
Reaction Conditions | 0.1, 0.5, 1, 5, 10, 50 and 100μM; 48h |
Applications | Dynorphin A (trifluoroacetate salt) treatment reduced viability of U2OS cells in a dose-dependent manner. |
References: | |
| Cas No. | SDF | Download SDF | |
| 别名 | Dynorphin A (1-17) | ||
| Canonical SMILES | O=C(N[C@@H](CC(O)=O)C(N[C@@H](CC(N)=O)C(N[C@H](C(O)=O)CCC(N)=O)=O)=O)[C@@H](NC([C@H](CCCCN)NC([C@H](CC(C)C)NC([C@H](CCCCN)NC([C@H](CCC1)N1C([C@H](CCCNC(N)=N)NC([C@@]([C@@H](C)CC)([H])NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC([C@H](CC(C)C)NC([C@@H](NC(CNC(CNC([C@@H](N)CC2=CC=C(O)C=C2)=O)=O)=O)CC3=CC=CC=C3)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CC4=CNC5=CC=CC=C45.FC(F)(C(O)=O)F | ||
| 分子式 | C99H155N31O23 ? XCF3COOH | 分子量 | 2147.5 |
| 溶解度 | DMF: 30 mg/mL,DMSO: 30 mg/mL,PBS (pH 7.2): 5 mg/mL | 储存条件 | -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 465.7 μL | 2.3283 mL | 4.6566 mL |
| 5 mM | 93.1 μL | 465.7 μL | 931.3 μL |
| 10 mM | 46.6 μL | 232.8 μL | 465.7 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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