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Art. -Nr.: HY-187342

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KOR modulator-1

KOR modulator-1 is a blood-brain barrier-permeable kappa opioid receptor (KOR) modulator. KOR modulator-1 induces antinociceptive effects without significant sedation or impairment of neuromuscular coordination. KOR modulator-1 can be used for the research of chronic pain.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₆H₂₇ClN₄O₂
Molecular Weight:462.97

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

KOR modulator-1 Chemical Structure

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

κ Opioid Receptor/KOR

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

KOR modulator-1 (15ao) (10 pM-10 μM) potently and selectively inhibits cAMP production via G-protein-dependent signaling in KOR-transfected HEK293T cells, with an IC₅₀ of 5.1 nM^[1].
KOR modulator-1 (10 pM-10 μM) induces β-arrestin 2 recruitment in HTLA cells expressing human KOR with an EC₅₀ of 191 nM, and exhibits extreme G-protein-biased signaling with a bias factor of 1.55^[1].
KOR modulator-1 (10 pM-10 μM) does not stimulate ERK1/2-MAPK signaling in KOR-transfected HEK293T cells^[1].
KOR modulator-1 binds to the orthosteric pocket of active-state human KOR with key conserved interactions and a predicted MM-GBSA binding affinity of -59.70 kcal/mol^[1].

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

Parmacokinetics

Species	Dose	Route	Note	T_1/2	T_max	C_max	AUC_{INF_obs}	MRT_{INF_obs}
Mice^[1]	5 mg/kg	s.c.	Plasma	7.81 h	1.10 h	3616.31 ng/mL	15715.99 ng·h/mL	7.19 h
Mice^[1]	5 mg/kg	s.c.	Brain	6.02 h	0.75 h	188.31 ng/mL	1352.23 ng·h/mL	12 h

In Vivo

KOR modulator-1 (15ao) (5 mg/kg; s.c.; single dose) produces significant antinociceptive activity in a mouse radiant heat pain model^[1].
KOR modulator-1 (5 mg/kg; s.c.; single dose) does not induce sedation in mice^[1].
KOR modulator-1 (5-10 mg/kg; s.c.; single dose) does not impair neuromuscular coordination in mice^[1].

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

Animal Model:

C57BL/6 (male)^[1]
Dosage:

5 mg/kg
Administration:

s.c.; single dose
Result:

Induced a time-dependent increase in %MPE, with efficacy clearly separated from vehicle over early to mid-time points.
Produced a significant increase in the area under the %MPE-time curve (AUC) relative to vehicle, approaching the efficacy of the reference agonist U50488.

Animal Model:

C57BL/6 (male)^[1]
Dosage:

5 mg/kg
Administration:

s.c.; single dose
Result:

Exhibited no significant suppression of locomotor activity compared to vehicle control, in contrast to the unbiased reference agonist U50488 and less biased compounds.

Animal Model:

C57BL/6 (male)^[1]
Dosage:

5 mg/kg; 10 mg/kg
Administration:

s.c.; single dose
Result:

Showed no significant reduction in rotarod fall latency at either 5 mg/kg or 10 mg/kg, in contrast to the unbiased reference agonist U50488 which caused a significant impairment.

Chemical Information

Molecular Weight 462.97
Formel C₂₆H₂₇ClN₄O₂
SMILES

CC(C)(C)NC(C(N1CC2=CC=CC=C2)C3=[N+](CC1=O)C=CC4=C3NC5=C4C=CC=C5)=O.[Cl-]
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Ghosh A, et al. Modular synthesis and bioevaluation of novel fused-β-carbolines as kappa opioid receptor modulators. European journal of medicinal chemistry. 2026 Jul 11;317:119119. [Content Brief]

Calculators

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)}

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.

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
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KOR modulator-1

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

KOR modulator-1 Related Classifications

HY-187342 Related Classifications