1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. ICI 174864

ICI 174864 is a highly selective, potent δ-receptor antagonist. ICI 174864 is equipotent with naloxone and can not reverse the effect of the μ-agonist [D-Ala2, MePhe4, Gly-Ol5]enkephalin or the κ-agonist-tifluadom.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

ICI 174864 Chemical Structure

ICI 174864 Chemical Structure

CAS No. : 89352-67-0

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1 mg USD 482 In-stock
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Description

ICI 174864 is a highly selective, potent δ-receptor antagonist. ICI 174864 is equipotent with naloxone and can not reverse the effect of the μ-agonist [D-Ala2, MePhe4, Gly-Ol5]enkephalin or the κ-agonist-tifluadom[1].

Cellular Effect
Cell Line Type Value Description References
CHO EC50
116 nM
Compound: ICI-174864
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
[PMID: 26048798]
CHO IC50
18900 nM
Compound: ICI-174864
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.
[PMID: 11052799]
CHO IC50
703 nM
Compound: ICI-174864
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.
[PMID: 11052799]
Molecular Weight

606.75

Formula

C34H46N4O6

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

{N,N-diallyl}-Tyr-{Aib}-Phe-Leu

Sequence Shortening

{N,N-diallyl}-Y-{Aib}-FL

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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ICI 174864
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