ICI 174864
Based on 1 Customer Validation
ICI 174864 is a selective and brain-penetrant δ-opioid receptor antagonist with Ke values of 22.0 nM to 30.6 nM at δ-opioid receptor in mouse vas deferens. ICI 174864 selectively blocks biological effects mediated by the δ-opioid receptor agonist DPDPE (HY-P1334) after central administration. ICI 174864 reverses hypotension in rats with endotoxic shock and inhibits acetic acid-induced writhing in mice. ICI 174864 can be used for the research of opioid receptor subtypes, endotoxic hypotension and analgesic pathways.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.84%
- CAS 番号: 89352-67-0
- 分子式: C34H46N4O6
- 分子量:606.75
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Deltorphin Iδ-Opioid Receptor Agonist -
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(-)-U-50488 hydrochlorideKOR Agonist
Opioid Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[2]|
δ Opioid Receptor/DOR |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
116 nM
Compound: ICI-174864
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Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay
Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay
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[PMID: 26048798] |
| CHO | IC50 |
18900 nM
Compound: ICI-174864
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Binding affinity was measured in cloned Opioid receptor mu 1 expressed in CHO cells using [3H]- DAMGO as radioligand.
Binding affinity was measured in cloned Opioid receptor mu 1 expressed in CHO cells using [3H]- DAMGO as radioligand.
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[PMID: 11052799] |
| CHO | IC50 |
703 nM
Compound: ICI-174864
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Binding affinity was measured in cloned Opioid receptor delta 1 expressed in CHO cells using [3H]- DPDPE as radioligand.
Binding affinity was measured in cloned Opioid receptor delta 1 expressed in CHO cells using [3H]- DPDPE as radioligand.
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[PMID: 11052799] |
体外実験
ICI 174864 selectively antagonizes delta opioid receptors in in vitro biochemical systems[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
ICI 174864 (10 μg; i.c.v.; single dose; 3-10 mg/kg; s.c.; single dose) induces dose-dependent behavioral depression and ptosis via s.c. administration, and postural abnormalities, barrel rotation, and hypothermia via i.c.v. administration in naive male Sprague Dawley rats[2].
ICI 174864 (10 μg; i.c.v.; single dose) suppresses acetic acid-induced writhing in male albino mice in a Naloxone-sensitive manner, while 5 μg (i.c.v.; single dose) selectively antagonizes the writhing-suppressant effect of delta agonist DPDPE (HY-P1334) without affecting mu agonist DAGO[2].
ICI 174864 (3μg; i.c.v.; single dose) completely blocks DADL-induced hyperphagia[3].
ICI 174864 (3 mg/kg; i.v.; single dose) significantly reverses endotoxic shock hypotension in male Sprague Dawley rats, without affecting blood pressure in normotensive rats[5].
ICI 174864 (3 mg/kg; i.v.; single dose) produces only a rapid, transient pressor response with no sustained effect in normotensive male Sprague Dawley rats[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (adult female, 200-220 g)[1]
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Dosage:1 μg (inconsistent δ-antagonism); 3 μg (selective δ-antagonism); 6 μg (agonistic activity); 15 μg (bladder contraction inhibition); 50 μg (lethal); 100 μg (lethal)
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Administration:i.c.v.; single dose
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Result:Produced inconsistent δ-receptor antagonism without affecting bladder contractions.
Completely and reversibly antagonized DPDPE-mediated bladder inhibition without altering DAGO effects.
Showed naloxone-resistant agonistic activity that inhibited bladder contractions.
Caused lethal effects in rats.
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Animal Model:Sprague Dawley albino rats (male, 200-220 g)[2]
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Dosage:10 μg (i.c.v.); 3 mg/kg (s.c.); 10 mg/kg (s.c.)
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Administration:i.c.v.; single dose; s.c.; single dose
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Result:Produced postural abnormalities, barrel rotation, prostration and behavioral depression.
Induced hypothermia in rats.
Caused dose-dependent behavioral depression and ptosis.
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Animal Model:albino mice (male, 22-30 g)[2]
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Dosage:10 μg (i.c.v.); 5 μg (i.c.v.); 3 mg/kg (s.c.)
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Administration:i.c.v.; single dose; s.c.; single dose
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Result:Suppressed acetic acid-induced writhing significantly.
Antagonized DPDPE-induced antinociception but not DAGO-induced antinociception.
Exhibited agonist activity attenuated by high-dose naloxone only.
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Animal Model:albino mice (male, 22-30 g)[2]
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Dosage:10 μg (i.c.v.); 25 μg (i.c.v.); 50 μg (i.c.v.)
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Administration:i.c.v.; single dose
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Result:Produced no obvious effect on tail flick latency.
Did not significantly antagonize analgesic effects of DPDPE or DAGO.
Weakly attenuated analgesic actions of DPDPE and DAGO without statistical significance.
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Animal Model:Sprague Dawley (male, 250-350 g, endotoxic shock model induced by E. coli lipopolysaccharide endotoxin 22.5 mg/kg i.v.)[5]
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Dosage:3 mg/kg
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Administration:i.v.; single dose
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Result:Produced a significant, sustained pressor effect following the initial transient spike, which was significantly greater than the vehicle control at relevant time points.
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Animal Model:Sprague Dawley (male, 250-350 g, normotensive)[5]
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Dosage:3 mg/kg
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Administration:i.v.; single dose
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Result:Produced a rapid, transient pressor response that disappeared within 5 minutes.
Showed no sustained pressor effect over the 60-minute period.
化学情報
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CAS 番号 89352-67-0
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性状 Solid
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分子量 606.75
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分子式 C34H46N4O6
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Color White to off-white
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配列
{N,N-diallyl}-Tyr-{Aib}-Phe-Leu
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シーケンスの短縮
{N,N-diallyl}-Y-{Aib}-FL
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (164.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Dray A, et al. Selective delta-opioid receptor antagonism by ICI 174,864 in the central nervous system. Peptides. 1984;5(5):1015-1016. [Content Brief]
[2]. van der Meer JW, et al. Abstract!. Neth J Med. 2002;60(11):418. [Content Brief]
[3]. Jackson HC, et al. Hyperphagia induced by 2-deoxy-D-glucose in the presence of the delta-opioid antagonist ICI 174,864. Neuropharmacology. 1985;24(8):815-817. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6481 mL | 8.2406 mL | 16.4813 mL | 41.2031 mL |
| 5 mM | 0.3296 mL | 1.6481 mL | 3.2963 mL | 8.2406 mL | |
| 10 mM | 0.1648 mL | 0.8241 mL | 1.6481 mL | 4.1203 mL | |
| 15 mM | 0.1099 mL | 0.5494 mL | 1.0988 mL | 2.7469 mL | |
| 20 mM | 0.0824 mL | 0.4120 mL | 0.8241 mL | 2.0602 mL | |
| 25 mM | 0.0659 mL | 0.3296 mL | 0.6593 mL | 1.6481 mL | |
| 30 mM | 0.0549 mL | 0.2747 mL | 0.5494 mL | 1.3734 mL | |
| 40 mM | 0.0412 mL | 0.2060 mL | 0.4120 mL | 1.0301 mL | |
| 50 mM | 0.0330 mL | 0.1648 mL | 0.3296 mL | 0.8241 mL | |
| 60 mM | 0.0275 mL | 0.1373 mL | 0.2747 mL | 0.6867 mL | |
| 80 mM | 0.0206 mL | 0.1030 mL | 0.2060 mL | 0.5150 mL | |
| 100 mM | 0.0165 mL | 0.0824 mL | 0.1648 mL | 0.4120 mL |
ICI 174864 関連分類
HY-101230 関連分類
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