Cat. No.: HY-12363

U-69593

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U-69593 is a potent and selective κ1-opioid receptor agonist. U-69593 attenuates addictive agent-induced behavioral sensitization in the rat. U-69593 reduces anxiety and enhances spontaneous alternation memory in mice. U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum.

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Pureté: 99.73%
CAS No.: 96744-75-1
Formule: C₂₂H₃₂N₂O₂
Masse moléculaire:356.50

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Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

U-69593 Chemical Structure

CAS No.: 96744-75-1

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
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Activité biologique

Description

U-69593 is a potent and selective κ1-opioid receptor agonist^[1]. U-69593 attenuates addictive agent-induced behavioral sensitization in the rat^[2]. U-69593 reduces anxiety and enhances spontaneous alternation memory in mice^[3]. U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum^[4].

IC₅₀ & Target

κ Opioid Receptor/KOR

Voir tous les produits spécifiques à Isoform Opioid Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	>10000 nM Compound: U-69593	Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells	[PMID: 12672258]
CHO	EC₅₀	26.1 nM Compound: U-69593	Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells. Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells.	[PMID: 12672258]
CHO	EC₅₀	>10000 nM Compound: U-69593	Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells. Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.	[PMID: 12672258]
CHO	EC₅₀	207 nM Compound: U-69593	Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding	[PMID: 16441078]
CHO	EC₅₀	6.6 nM Compound: U-69593	Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay	[PMID: 16441078]
CHO	EC₅₀	207 nM Compound: U-69593	Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	[PMID: 17580847]
CHO	EC₅₀	12.5 nM Compound: U-69593	Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as calcium mobilization after 1 hrs by fluorescence analysis Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as calcium mobilization after 1 hrs by fluorescence analysis	[PMID: 22464684]
CHO	EC₅₀	26.1 nM Compound: U69,593	Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay	[PMID: 23134120]
CHO	EC₅₀	28.1 nM Compound: U-69,593	Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells after 2 hrs by [35S]-GTPgammaS binding assay Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells after 2 hrs by [35S]-GTPgammaS binding assay	[PMID: 23200250]
CHO	EC₅₀	60.14 nM Compound: U69593	Agonist activity at human kappa opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis Agonist activity at human kappa opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	[PMID: 24657054]
CHO	EC₅₀	12 nM Compound: U-69,593	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding	[PMID: 25147605]
CHO	EC₅₀	7.7 nM Compound: U69593	Agonist activity at rat kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at rat kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 25221662]
CHO	EC₅₀	8.03 nM Compound: U-69,593	Agonist activity at human KOR expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at human KOR expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 25248680]
CHO	EC₅₀	28.1 nM Compound: U-69,593	Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 25283554]
CHO	EC₅₀	0.8 nM Compound: U69,593	Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay	[PMID: 25426797]
CHO	EC₅₀	28.1 nM Compound: U-69593	Agonist activity at human KOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay Agonist activity at human KOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay	[PMID: 26346669]
CHO	IC₅₀	0.63 nM Compound: U-69593	Binding affinity against rat kappa-opioid receptor expressed in CHO cells was determined by competitive inhibition of 2 nM [3H]-U 69593 Binding affinity against rat kappa-opioid receptor expressed in CHO cells was determined by competitive inhibition of 2 nM [3H]-U 69593	[PMID: 9873480]
HEK293	ED₅₀	24 nM Compound: U-69593	Effective dose for agonistic activity towards human kappa opioid receptor from membranes of HEK293 cells was determined by radiolabeled [35S]GTP-gamma-S, assay Effective dose for agonistic activity towards human kappa opioid receptor from membranes of HEK293 cells was determined by radiolabeled [35S]GTP-gamma-S, assay	[PMID: 12643930]
HEK293	IC₅₀	2 nM Compound: U-69593	Inhibition of [125I]-(D-Pro10)-Dynorphin A binding to human kappa opioid receptor from membranes of HEK293 cells Inhibition of [125I]-(D-Pro10)-Dynorphin A binding to human kappa opioid receptor from membranes of HEK293 cells	[PMID: 12643930]
HEK293	IC₅₀	250 nM Compound: U-69593	Inhibition of [125I]Enkephalin binding to human mu opioid receptor from membranes of HEK293 cells Inhibition of [125I]Enkephalin binding to human mu opioid receptor from membranes of HEK293 cells	[PMID: 12643930]
HEK293	IC₅₀	5800 nM Compound: U-69593	Inhibition of [125I]deltorphin binding to human delta opioid receptor from membranes of HEK293 cells Inhibition of [125I]deltorphin binding to human delta opioid receptor from membranes of HEK293 cells	[PMID: 12643930]
HEK293	EC₅₀	11 nM Compound: U-69593	Agonist activity at human kappa opioid receptor in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding Agonist activity at human kappa opioid receptor in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding	[PMID: 18637671]
HEK293	IC₅₀	8 nM Compound: U-69593	Displacement of [3H]naloxone from kappa opioid receptor expressed in HEK293 cell membrane Displacement of [3H]naloxone from kappa opioid receptor expressed in HEK293 cell membrane	[PMID: 20426456]
HEK293	EC₅₀	80 nM Compound: U-69593	Agonist activity at human recombinant kappa opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 45 mins by microplate luminescence assay Agonist activity at human recombinant kappa opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 45 mins by microplate luminescence assay	[PMID: 20441176]
HEK293	EC₅₀	534 nM Compound: U69593	Agonist activity at GFP-fused kappa opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay Agonist activity at GFP-fused kappa opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay	[PMID: 24613457]
HEK293	EC₅₀	80 nM Compound: U-69593	Agonist activity at recombinant kappa-opioid receptor in human HEK293 cells by [35S]-GTP-gammaS binding assay Agonist activity at recombinant kappa-opioid receptor in human HEK293 cells by [35S]-GTP-gammaS binding assay	[PMID: 24856182]
HEK293	EC₅₀	12 nM Compound: U-69593	Agonist activity at human kappa opioid receptor expressed in HEK-293 cells assessed as stimulation of [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting analysis Agonist activity at human kappa opioid receptor expressed in HEK-293 cells assessed as stimulation of [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting analysis	[PMID: 25062506]
HEK293	EC₅₀	5.3 nM Compound: U-69,593	Agonist activity at recombinant human kappa-type opioid receptor expressed in HEK293 cells after 30 mins by [35S]GTPgammaS binding assay Agonist activity at recombinant human kappa-type opioid receptor expressed in HEK293 cells after 30 mins by [35S]GTPgammaS binding assay	[PMID: 28218838]
HEK293	EC₅₀	12 nM Compound: U-69593	Agonist activity at human kappa opioid receptor expressed in HEK-293 cells after 45 mins by [35S]GTP-gamma-S binding assay in presence of 10 uM of GDP Agonist activity at human kappa opioid receptor expressed in HEK-293 cells after 45 mins by [35S]GTP-gamma-S binding assay in presence of 10 uM of GDP	10.1039/C5MD00414D
U2OS	EC₅₀	131 nM Compound: U69,593	Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with EFC and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by luminescence assay Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with EFC and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by luminescence assay	[PMID: 29939744]
U2OS	EC₅₀	205 nM Compound: U69,593	Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with GFP and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 20 mins by Hoechst staining-based assay Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with GFP and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 20 mins by Hoechst staining-based assay	[PMID: 29939744]
U2OS	EC₅₀	5.4 nM Compound: U69,593	Agonist activity at human kappa opioid receptor expressed in human U2OS cells assessed as increase in ERK1/2 phosphorylation after 10 mins by Western blot analysis Agonist activity at human kappa opioid receptor expressed in human U2OS cells assessed as increase in ERK1/2 phosphorylation after 10 mins by Western blot analysis	[PMID: 29939744]

In Vivo

U-69593 (0.16 mg/kg; s.c.) attenuates addictive agent-induced behavioral sensitization in the rat^[2].
U-69593 (1, 10, 25 nmol/μL; Microinjection) reduces anxiety and enhances spontaneous alternation memory in mice^[3].
U-69593 (0.32 mg/kg; s.c.) decreases acute amphetamine-evoked behaviors and calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Rat^[2]
Dosage:

0.16 mg/kg
Administration:

S.c. (an acute injection of cocaine (20 mg/kg i.p.))
Result:

Attenuated the acute and chronic effects of cocaine on locomotor activity and stereotypy.

Animal Model:

CD-1 mice^[3]
Dosage:

1, 10, 25 nmol/µL
Administration:

Microinjection (in the infralimbic cortex (IL)), once every week, 2 weeks
Result:

Dose-dependently prolonged transfer-latency (T-L) and produced a dose-dependent anxiolytic behavioural profile, and after 24 h, the mouse were observed small but detectable carry-over effects. In week 2, U-69593 dose-dependently prolonged T/L and produced an anxiolytic behavioural profile in the first EPM (elevated plus-maze) trial, but observed a robust anxiolytic behavioural profile.

Animal Model:

280-350 g, male Wistar rats^[4]
Dosage:

0.32 mg/kg
Administration:

S.c. (followed 15 min later by an injection of amphetamine (2.5 mg/kg i.p.))
Result:

Significantly reduced the amphetamine-stimulated increase in dialysate dopamine levels and blocked the ability of amphetamine to evoke an increase in dialysate glutamate levels.

Chemical Information

CAS No. 96744-75-1
Appearance Solid
Masse moléculaire 356.50
Formule C₂₂H₃₂N₂O₂
Color White to off-white
SMILES

CN([C@@H]1[C@](N2CCCC2)([H])C[C@]3(CCCO3)CC1)C(CC4=CC=CC=C4)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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J Med Chem

2026 Mar 5;69(6):6508-6527.

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (140.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : 10 mg/mL (28.05 mM; Need ultrasonic and warming)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8050 mL

14.0252 mL

28.0505 mL

5 mM

0.5610 mL

2.8050 mL

5.6101 mL

10 mM

0.2805 mL

1.4025 mL

2.8050 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Elemental Analysis Report (2659 KB)
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Instruction de manipulation (2659 KB)

Références

[1]. Lahti RA, et al. [3H]U-69593 a highly selective ligand for the opioid kappa receptor. Eur J Pharmacol. 1985 Feb 26;109(2):281-4. [Content Brief]

[2]. [2]Heidbreder CA, et al. The kappa-opioid receptor agonist U-69593 attenuates cocaine-induced behavioral sensitization in the rat. Brain Res. 1993 Jul 9;616(1-2):335-8. [Content Brief]

[3]. [3]Wall PM, et al. U-69,593 microinjection in the infralimbic cortex reduces anxiety and enhances spontaneous alternation memory in mice. Brain Res. 2000 Feb 21;856(1-2):259-80. [Content Brief]

[4]. [4]Gray AM, et al. The kappa-opioid agonist, U-69593, decreases acute amphetamine-evoked behaviors and calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum. J Neurochem. 1999 Sep;73(3):1066-74. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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
DMF / DMSO	1 mM	2.8050 mL	14.0252 mL	28.0505 mL	70.1262 mL
	5 mM	0.5610 mL	2.8050 mL	5.6101 mL	14.0252 mL
	10 mM	0.2805 mL	1.4025 mL	2.8050 mL	7.0126 mL
	15 mM	0.1870 mL	0.9350 mL	1.8700 mL	4.6751 mL
	20 mM	0.1403 mL	0.7013 mL	1.4025 mL	3.5063 mL
	25 mM	0.1122 mL	0.5610 mL	1.1220 mL	2.8050 mL
DMSO	30 mM	0.0935 mL	0.4675 mL	0.9350 mL	2.3375 mL
	40 mM	0.0701 mL	0.3506 mL	0.7013 mL	1.7532 mL
	50 mM	0.0561 mL	0.2805 mL	0.5610 mL	1.4025 mL
	60 mM	0.0468 mL	0.2338 mL	0.4675 mL	1.1688 mL
	80 mM	0.0351 mL	0.1753 mL	0.3506 mL	0.8766 mL
	100 mM	0.0281 mL	0.1403 mL	0.2805 mL	0.7013 mL

Keywords

U-69593

1 Cited Publications

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U-69593

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) U-69593

Voir tous les produits spécifiques à Isoform Opioid Receptor

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

U-69593

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) U-69593

Voir tous les produits spécifiques à Isoform Opioid Receptor

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

U-69593 Related Classifications

HY-12363 Related Classifications