| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
delta-opioid receptor (DOR). ICI 174,864 is a highly selective delta opioid receptor antagonist. It shows no antagonist activity at micro and kappa receptors, making it a valuable tool for discriminating delta-receptor-mediated effects. At high concentrations, it exhibits partial agonist activity at delta receptors.
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| ln Vitro |
ICI 174,864 is a selective delta receptor antagonist. It is equivalent to naloxone in potency at delta receptors but does not reverse the effects of micro agonists (e.g., [D-Ala2, MePhe4, Gly-Ol5] enkephalin) or kappa agonists (tifluadom). At high concentrations, it exhibits partial agonist activity at delta receptors in vitro, meaning it can produce weak delta-mediated effects under certain conditions. No specific IC50 or Ki values are provided.
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| ln Vivo |
No specific in vivo activity data are reported for ICI 174,864. As a selective delta receptor antagonist, it is used to block delta opioid receptor-mediated effects in vivo, including analgesia, convulsant activity, and gastrointestinal motility. It is particularly useful for studying the role of delta receptors in opioid-induced effects without affecting micro and kappa receptor signaling. Its in vivo duration of action is moderate (hours).
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| Enzyme Assay |
Cell-free delta-opioid receptor binding assays are performed using membranes from CHO-K1 cells stably expressing the human delta-opioid receptor or from mouse brain (minus cerebellum). Membranes are incubated with a delta-selective radioligand (e.g., [3H]-naltrindole, 0.5-1 nM, or [3H]-DPDPE, 1-2 nM) and increasing concentrations of ICI 174,864 (0.01-10,000 nM) in 50 mM Tris-HCl (pH 7.4) containing 1 mM EDTA, 5 mM MgCl2, and 0.1% BSA for 60-90 min at 25degC. Bound radioactivity is separated by GF/B filtration. IC50 and Ki are calculated by nonlinear regression. Selectivity is confirmed using micro-selective ([3H]-DAMGO) and kappa-selective ([3H]-U69,593) radioligands in separate experiments. ICI 174,864 is highly selective for delta over micro and kappa.
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| Cell Assay |
Cell-based functional assays: CHO-K1 cells stably expressing the human delta-opioid receptor are loaded with a cAMP detection kit (HTRF). ICI 174,864 is pre-incubated with the cells for 10-15 min at increasing concentrations (0.1-10,000 nM), followed by stimulation with a delta agonist (e.g., DPDPE 1-100 nM) in the presence of forskolin (10 uM). The ability of ICI 174,864 to reverse agonist-induced inhibition of cAMP accumulation is measured. IC50 for antagonist activity is determined. At high concentrations (>1 uM), ICI 174,864 may produce weak cAMP inhibition (partial agonist activity). For selectivity assessment, the same assay is performed using cells expressing micro or kappa receptors; ICI 174,864 does not reverse micro or kappa agonist-induced effects at concentrations up to 10 uM.
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| Animal Protocol |
No specific published in vivo animal protocols are available for ICI 174,864. Standard protocols: ICI 174,864 is dissolved in 0.9% saline or 10% DMSO in saline and administered i.c.v. (1-20 ug/mouse), i.t. (0.5-10 ug/mouse), or i.p. (1-10 mg/kg) in rodents 10-30 min prior to delta agonist challenge. Analgesia is assessed by tail-flick or hot-plate tests. Antagonist activity is confirmed by rightward shift of the delta agonist dose-response curve. For gastrointestinal motility studies, intestinal transit is measured after charcoal meal administration. For convulsant activity, seizure latency and severity are recorded after delta agonist administration. The compound‘s selectivity in vivo can be confirmed by lack of antagonism of micro or kappa agonists in tail-flick tests.
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| ADME/Pharmacokinetics |
No specific pharmacokinetic data are reported for ICI 174,864. The molecular weight is 691.87 (C38H53N5O7). CAS# 89352-67-0. Purity ≥95%. ICI 174,864 is a synthetic peptide and is not orally bioavailable. For in vivo studies, it is typically administered by intracerebroventricular or intrathecal injection to achieve CNS concentrations. Following central administration, the half-life is short (minutes to hours) due to enzymatic degradation in brain tissue. Peripheral administration (i.p.) may result in poor CNS penetration. Solubility: DMSO, 10-50 mg/mL. Storage: -20degC, dry, away from moisture.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for ICI 174,864. At doses used in published studies (i.c.v. up to 20 ug/mouse, i.p. up to 10 mg/kg), no overt signs of toxicity (seizures, respiratory depression, death) have been reported. However, comprehensive toxicological assessments (Ames, hERG, repeat-dose) have not been performed. ICI 174,864 has not advanced to clinical trials and is not FDA-approved. For research use only.
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| References | |
| Additional Infomation |
Other information: ICI 174,864 is a research-grade selective delta-opioid receptor antagonist (CAS# 89352-67-0), not FDA-approved. It is a synthetic peptide (N,N-diallyl-Tyr-Aib-Aib-Phe-Leu-OH, where Aib = aminoisobutyric acid). It exhibits partial agonist activity at delta receptors at high concentrations. It is a valuable tool for delta opioid receptor pharmacology studies, including investigations of opioid analgesia, tolerance, dependence, and gastrointestinal function. Sold with the permission of AstraZeneca UK Ltd. For research use only.
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| Molecular Formula |
C34H46N4O6
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|---|---|
| Molecular Weight |
606.75
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| Exact Mass |
691.394
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| CAS # |
89352-67-0
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| PubChem CID |
44149909
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| Appearance |
White to off-white solid powder
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| Density |
1.16 g/cm3
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| Boiling Point |
892.7ºC at 760 mmHg
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| Flash Point |
493.7ºC
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| Index of Refraction |
1.564
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| LogP |
4.673
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
50
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| Complexity |
1160
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C(O)(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@](C)(C)NC(=O)[C@H](CC1=CC=C(O)C=C1)N(CC=C)CC=C
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| InChi Key |
XUWLAGNFLUARAN-CHQNGUEUSA-N
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| InChi Code |
InChI=1S/C38H53N5O7/c1-9-20-43(21-10-2)31(24-27-16-18-28(44)19-17-27)33(46)41-38(7,8)36(50)42-37(5,6)35(49)40-29(23-26-14-12-11-13-15-26)32(45)39-30(34(47)48)22-25(3)4/h9-19,25,29-31,44H,1-2,20-24H2,3-8H3,(H,39,45)(H,40,49)(H,41,46)(H,42,50)(H,47,48)/t29-,30-,31-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[bis(prop-2-enyl)amino]-3-(4-hydroxyphenyl)propanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6481 mL | 8.2406 mL | 16.4813 mL | |
| 5 mM | 0.3296 mL | 1.6481 mL | 3.2963 mL | |
| 10 mM | 0.1648 mL | 0.8241 mL | 1.6481 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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