Art. -Nr.: HY-15997

(-)-U-50488 hydrochloride

(Synonyms: (-)-Trans-(1S,2S)-U-50488 hydrochloride)

1 Cited Publications

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(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (K_d=2.2 nM) over μ-opioid receptor (MOR) (K_d=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+) trans-(1R,2R) U-50488 (HY-15997A) or the (±) trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM).

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Reinheit: 98.95%
CAS. Nr.: 114528-79-9
Formel: C₁₉H₂₇Cl₃N₂O
Molecular Weight:405.79

Speicherung:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

(-)-U-50488 hydrochloride Chemical Structure

CAS. Nr.: 114528-79-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Kd: 2.2 nM (kappa-opioid receptor (KOR))
Kd: 430 nM (μ-opioid receptor (MOR))^[1]

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	17 nM Compound: U50,488H	Agonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis Agonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis	[PMID: 27556704]
CHO	EC₅₀	35.8 nM Compound: U50488	Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	[PMID: 32530286]
HEK293	EC₅₀	0.4 nM Compound: 16	Activity at kappa opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding Activity at kappa opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding	[PMID: 19683449]

In Vitro

(-)-U-50488 hydrochloride (1 pM-100 nM; 7 days) exhibits a concentration-dependent inhibition of HIV-1 expression, the maximal inhibition at 10 13 M (approximately 73% suppression) in acutely infected blood monocyte-derived macrophages (MDM)^[2].
(-)-U-50488 hydrochloride (10^-13 M; 7-14 days) (10 13 M) markedly inhibits HIV-1 expression both at 7 and 14 days after infection, it has a sustained inhibitory effect on HIV-1 infection in MDM^[2].

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

In Vivo

(-)-U-50488 hydrochloride (intraperitoneal injection; 5mg/kg; 2 hrs before 4% paraformaldehyde (PFA)) acutely induced pMeCP2-S421 (phosphorylation of the methyl-DNA binding protein MeCP2 at Ser421) and Fos selectively in the nucleus accumbens (NAc) but does not alter MeCP2 levels in any brain region^[3].

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

Animal Model:

C57BL/6J mice^[1]
Dosage:

5 mg/kg
Administration:

Intraperitoneal injection; single dose; 2 hrs before 4% PFA
Result:

Induced pMeCP2-S421 in the brain acutely.

Chemical Information

CAS. Nr. 114528-79-9
Appearance Solid
Molecular Weight 405.79
Formel C₁₉H₂₇Cl₃N₂O
Color White to off-white
SMILES

O=C(N(C)[C@@H]1[C@@H](N2CCCC2)CCCC1)CC3=CC=C(Cl)C(Cl)=C3.[H]Cl
Synonyms

(-)-Trans-(1S,2S)-U-50488 hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Publications (1)

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Journal Impact Factor

ACS Cent Sci

An Epigenetic Switch for Sex-Specific Brain Resilience in Stroke: Targeting HDAC2 to Amplify Endogenous Oxytocin Signaling. [Abstract]

2026 Mar 25;12(4):497-523. PMID: 42038487

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (246.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (123.22 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

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

2.4643 mL

12.3216 mL

24.6433 mL

5 mM

0.4929 mL

2.4643 mL

4.9287 mL

10 mM

0.2464 mL

1.2322 mL

2.4643 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (6.16 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 (6.16 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.16 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Reinheit & Dokumentation

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Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
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- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kirti Kumari Sharma, et al. The search for the "next" euphoric non-fentanil novel synthetic opioids on the illicit drugs market: current status and horizon scanning. Forensic Toxicol. 2019;37(1):1-16. [Content Brief]

[2]. Anthony S Zannas, ET AL. Regulation and function of MeCP2 Ser421 phosphorylation in U50488-induced conditioned place aversion in mice. Psychopharmacology (Berl). 2017 Mar;234(6):913-923. [Content Brief]

[3]. C C Chao,et al. U50488 inhibits HIV-1 expression in acutely infected monocyte-derived macrophages. Drug Alcohol Depend. 2001 Apr 1;62(2):149-54. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.4643 mL	12.3216 mL	24.6433 mL	61.6082 mL
	5 mM	0.4929 mL	2.4643 mL	4.9287 mL	12.3216 mL
	10 mM	0.2464 mL	1.2322 mL	2.4643 mL	6.1608 mL
	15 mM	0.1643 mL	0.8214 mL	1.6429 mL	4.1072 mL
	20 mM	0.1232 mL	0.6161 mL	1.2322 mL	3.0804 mL
	25 mM	0.0986 mL	0.4929 mL	0.9857 mL	2.4643 mL
	30 mM	0.0821 mL	0.4107 mL	0.8214 mL	2.0536 mL
	40 mM	0.0616 mL	0.3080 mL	0.6161 mL	1.5402 mL
	50 mM	0.0493 mL	0.2464 mL	0.4929 mL	1.2322 mL
	60 mM	0.0411 mL	0.2054 mL	0.4107 mL	1.0268 mL
	80 mM	0.0308 mL	0.1540 mL	0.3080 mL	0.7701 mL
	100 mM	0.0246 mL	0.1232 mL	0.2464 mL	0.6161 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

(-)-U-50488 hydrochloride

1 Cited Publications

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(-)-U-50488 hydrochloride

Publications Citing Use of MedChemExpress (MCE) (-)-U-50488 hydrochloride

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

(-)-U-50488 hydrochloride Related Classifications

HY-15997 Related Classifications