[D-Ala2]-Deltorphin II
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
[D-ALA2] -deltorphin II(DADELT II)是δ阿片受体的一种天然激动剂,Ki或IC50值为0.41 nM [1,2]。
阿片受体在中枢神经系统广泛分布,但也存在于哺乳动物许多外周组织。主要有三种类型的阿片受体,即μ、δ和κ受体[2]。
[D-Pen2, D-Pen5]脑啡肽(DPDPE)为δ受体的第二个高选择性激动剂[3]。在NG108-15细胞中,短短3分钟1 M的DPDPE治疗显著减少了阿片受体对环磷酸腺苷生成的抑制作用,这意味着神经δ阿片受体经历了快速脱敏,这种脱敏与激动剂刺激后3分钟内δ阿片受体的磷酸化时间短暂平行[4]。
0.38-12.78 nM浓度DADELT II 经I.c.v.给药以剂量和时间相关的方式发挥镇痛作用。DADELT II给药后10分钟,观察到最大止痛效应。直到DADELT II给药后60分钟,检测到药物的镇痛效果。DADELT II可以被选择性δ拮抗剂ICI 174864拮抗[3]。在大鼠脊髓以上和脊髓侧脑室给药后,0.2、1和10 μg/rat 的DADELT II以剂量相关方式抑制腹泻和结肠排珠,但没有影响小肠转运的速率。相同剂量的脊柱施用给药DADELT II产生类似的结果。纳曲吲哚(Naltrindole)是δ阿片受体的选择性拮抗剂。用1和10 mg/kg的纳曲吲哚皮下预处理可起到部分地和完全地拮抗DADELT II的功效[1]。
参考文献:
[1]. Broccardo M, Improta G. Antidiarrheal and colonic antipropulsive effects of spinal and supraspinal administration of the natural δ opioid receptor agonist,[D-Ala2] deltorphin II, in the rat. European journal of pharmacology, 1992, 218(1): 69-73.
[2]. Janecka A, Fichna J, Janecki T. Opioid receptors and their ligands. Current topics in medicinal chemistry, 2004, 4(1): 1-17.
[3]. Jiang Q, Mosberg HI, Porreca F. Antinociceptive effects of [D-Ala2] deltorphin II, a highly selective δ agonist in vivo. Life sciences, 1990, 47(11): PL43-PL47.
[4]. Cai Y, Zhang Y, Wu Y, et al. δ opioid receptor in neuronal cells undergoes acute and homologous desensitization. Biochemical and biophysical research communications, 1996, 219(2): 342-347.
Physical Appearance | White lyophilised solid |
Storage | Desiccate at -20°C |
M.Wt | 782.89 |
Cas No. | 122752-16-3 |
Formula | C38H54N8O10 |
Solubility | Soluble to 1 mg/ml in 10% acetonitrile |
Chemical Name | (S)-5-(((R)-1-(((S)-1-((2-amino-2-oxoethyl)amino)-3-methyl-1-oxobutan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)amino)-4-((S)-2-((R)-2-((S)-2-amino-3-(4-hydroxyphenyl)propanamido)propanamido)-3-phenylpropanamido)-5-oxopentanoic acid |
SDF | Download SDF |
Canonical SMILES | O=C([C@@H](C(C)C)NC([C@H](CCC(O)=O)NC([C@H](CC1=CC=CC=C1)NC([C@@H](C)NC([C@H](CC(C=C2)=CC=C2O)N)=O)=O)=O)=O)N[C@H](C(NCC(N)=O)=O)C(C)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
化学结构
![[D-Ala2]-Deltorphin II](http://www.apexbt.com//media/diy/images/struct/B5072.png)