[D-Ala2]-Deltorphin II
(Synonyms: [D-Ala2]-Deltorphin II) 目录号 : GC11848
[D-Ala2]-Deltorphin II 是 δ 的选择性肽激动剂；阿片受体。
![[D-Ala2]-Deltorphin II Chemical Structure](/media/struct/GC1/GC11848.png "[D-Ala2]-Deltorphin II Chemical Structure")
Cas No.:122752-16-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
[D-Ala2]-deltorphin II (DADELT II) is a natural agonist of δ opioid receptor with Ki or IC50 value of 0.41 nM [1, 2].
Opioid receptors are most abundant in the central nervous system, but are also localized in many peripheral tissues in mammalian organisms. there are three types of opioid receptors that are well-defined; the µ, δ and κ receptors [2].
[D-Pen2, D-Pen5]enkephalin (DPDPE) is a second highly selective agonist of δ [3]. Treatment with DPDPE at 1 M for as short as 3 min significantly diminished the inhibition of the opioid receptor in NG108-15 cells to cyclic AMP production. That means neuronal delta opioid receptor underwent acute desensitization. This desensitization was temporally parallel to the phosphorylation of delta opioid receptor 3 min. after agonist stimulation [4].
I.c.v. administration of DADELT II from 0.38-12.78 nM resulted in a dose- and time-related antinociception. 10 min after the administration of DADELT II, the maximal antinociceptive response was seen. Until 60 min after the administration of DADELT II, effects were detected. These antinociceptive effects of i.c.v. DADELT II were antagonized by the selective δ antagonist, ICI 174,864 [3]. After supraspinal and spinal administration in rats intracerebroventricularly, DADELT II at 0.2, 1, 10 μg/rat in a dose-related fashion inhibited diarrhea and colonic bead expulsion but did not show any effect on the rate of small intestine transit. Spinal administration of DADELT II at the same dose produced similar results. Naltrindole is a selective antagonist of the δ opioid receptor. Subcutaneous pretreatment with naltrindole at 1 and 10 mg/kg antagonized effects of DADELT II partially and completely, respectively [1].
References:
[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.
| Cas No. | 122752-16-3 | SDF | |
| 别名 | [D-Ala2]-Deltorphin II | ||
| 化学名 | (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 | ||
| 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 | ||
| 分子式 | C38H54N8O10 | 分子量 | 782.89 |
| 溶解度 | Soluble to 1 mg/ml in 10% acetonitrile | 储存条件 | Desiccate at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2773 mL | 6.3866 mL | 12.7732 mL |
| 5 mM | 0.2555 mL | 1.2773 mL | 2.5546 mL |
| 10 mM | 0.1277 mL | 0.6387 mL | 1.2773 mL |
| 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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
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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