[D-Ala2]-Deltorphin II (Synonyms: [D-Ala2]-Deltorphin II) |
| カタログ番号GC11848 |
[D-Ala2]-デルトルフィン II は、δ に対する選択的ペプチド アゴニストです。オピオイド受容体。
Products are for research use only. Not for human use. We do not sell to patients.
![[D-Ala2]-Deltorphin II 化学構造](/media/struct/GC1/GC11848.png "[D-Ala2]-Deltorphin II 化学構造")
Cas No.: 122752-16-3
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
[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 | |
| 同義語 | [D-Ala2]-Deltorphin II | ||
| 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 | ||
| 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 | ||
| Formula | C38H54N8O10 | M.Wt | 782.89 |
| 溶解度 | Soluble to 1 mg/ml in 10% acetonitrile | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *