Art. -Nr.: HY-15481

KU14R

Name: KU14R
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SKU: HY-15481
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KU14R, an imidazole analog of efaroxan, is a putative imidazoline I3 receptor antagonist and reversible K_ATP channel inhibitor. KU14R inhibits K_ATP channel activity in mouse pancreatic β cells with an IC₅₀ of 31.9 μmol/L, and also suppresses Kir6.2 ΔC26 channel activity. KU14R exerts model-dependent antagonistic effects on imidazoline-sensitive insulin secretion. KU14R can be used in the research of diabetes-related diseases.

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Reinheit : 98.91%
CAS. Nr.: 189224-48-4
Formel: C₁₃H₁₄N₂O
Molecular Weight:214.26

Speicherung:

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

KU14R Chemical Structure

CAS. Nr.: 189224-48-4

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

K_ATP channel

31.9 μM (IC₅₀)

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In Vitro

OthersCarbohydrate MetabolismLocal Vascular Regulation

Others

KU14R (300 μM; doses to determine IC₅₀) potently blocks K_ATP channels in primary mouse pancreatic β cells, with an IC₅₀ of 31.9 μM, and achieves nearly complete inhibition at 300 μM^[1].
KU14R (100 μM) inhibits the Kir6.2 ΔC26 channel expressed in HEK cells, reducing channel activity to 45.2% of that in the control group at 100 μM^[1].
KU14R (100 μM) depolarizes the membrane potential of mouse pancreatic β cells to -33.4 mV, and fails to repolarize cells that have been depolarized by efaroxan^[1].
KU14R (100 μM; 30 min) does not alter cAMP levels in rat islets, nor does it reduce the forskolin (5 μM)- or IBMX (50 μM)-induced elevation of cAMP, suggesting that the antagonistic effect of KU14R on cAMP-dependent enhancement of insulin secretion occurs downstream of cAMP generation^[4].
KU14R (10^-5 M and 10^-4 M; pre-incubated for 10 min) antagonizes the response of the α2-adrenoceptor agonist UK14304 in isolated mouse vas deferens functional assays, with K_i values of 4.44 × 10^-6 M and 4.14 × 10^-6 M, respectively; KU14R (10^-6-10^-5 M) does not alter the concentration-response curve of the imidazoline ligand S22068^[2].

Carbohydrate Metabolism

KU14R (30-300 μM) barely potentiates glucose-induced insulin secretion in freshly isolated islets from NMRI mice; when glucose increases from 5 mmol/L to 10 mmol/L, the integrated insulin secretion in the presence of KU14R reaches 226% of the pre-stimulation level, and 100 μM KU14R does not antagonize efaroxan (100 μM)-induced insulin secretion^[1].
KU14R (0.1-1 μM; 7 mM glucose) dose-dependently reduces morin- or efaroxan-induced insulin secretion in MIN6 cells without altering basal insulin secretion; treatment with KU14R alone up to 50 μM also does not significantly change basal insulin secretion^[3].
KU14R (1 μM; 20 mM glucose) inhibits the further enhancing effect of morin (1 μM) on high glucose-induced insulin secretion, while KU14R alone does not reduce insulin secretion induced by 20 mM glucose^[3].
KU14R (100 μM; 1 h) does not alter basal insulin secretion induced by 6 or 20 mmol/L glucose in freshly isolated Wistar rat islets, but significantly inhibits the potentiating effects of efaroxan (100 μM), IBMX (50 μM) or forskolin (5 μM) on insulin secretion^[4].
KU14R itself does not alter insulin secretion from isolated islets of Wistar rats under 4-20 mM glucose conditions, but dose-dependently reverses the insulinotropic effect of efaroxan, exhibiting functional antagonism^[5].

Local Vascular Regulation

KU14R (1-100 μM; 10 min) exhibits weak α₂-adrenoceptor antagonist activity in isolated mouse vas deferens. It significantly and competitively inhibits UK14304-induced twitch suppression at concentrations of 10 μM and 100 μM, and directly suppresses twitches at 100 μM^[2].

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

ELISA Assay^[3]

Cell Line:

MIN6 cells (mouse-derived pancreatic β-cell line)
Concentration:

0.1 μM; 1 μM
Incubation Time:

30 min
Result:

Dose-dependently reduced morin- and efaroxan-induced insulin secretion without affecting basal insulin secretion.

ELISA Assay^[3]

Cell Line:

MIN6 cells (mouse-derived pancreatic β-cell line)
Concentration:

1 μM
Incubation Time:

2 h
Result:

Blocked morin-enhanced insulin secretion under high-glucose conditions without affecting insulin secretion induced by high glucose alone.

ELISA Assay^[3]

Cell Line:

MIN6 cells (mouse-derived pancreatic β-cell line)
Concentration:

50 μM
Incubation Time:

30 min pretreatment followed by 1 h incubation
Result:

Did not significantly alter basal insulin secretion.

In Vivo

Carbohydrate Metabolism

KU14R (4-25 mg/kg; i.p.; single dose) induces dose-dependent hypoglycemia in healthy male CBA/Ca mice, with an ED₅₀ of 16 mg/kg, and the response at 20 mg/kg involves increased plasma insulin levels^[2].
KU14R (16 mg/kg; i.p.; single dose) does not act as an antagonist of the hypoglycemic effect of S22068 (24 mg/kg) in healthy male CBA/Ca mice^[2].

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

Animal Model:

CBA/Ca (male, 16 weeks or older, 30-34 g)^[2]
Dosage:

4-25 mg/kg
Administration:

i.p.; single dose
Result:

Had no effect at 4 mg/kg.
Produced dose-dependent hypoglycemic responses at higher doses, with maximal decreases in blood glucose observed at 20-25 mg/kg between 120 and 180 min.
The median effective dose was 16 mg/kg.

Animal Model:

CBA/Ca (male, 16 weeks or older, 30-34 g)^[2]
Dosage:

20 mg/kg
Administration:

i.p.; single dose
Result:

Decreased blood glucose and significantly increased plasma insulin at 120 min.
Blood glucose had already decreased at 60 min, preceding the measurable increase in plasma insulin.

Animal Model:

CBA/Ca (male, 16 weeks or older, 30-34 g)^[2]
Dosage:

16 mg/kg
Administration:

i.p.; administered 60 min before Efaroxan
Result:

Produced a significantly greater and more prolonged decrease in blood glucose than efaroxan alone; blood glucose remained significantly reduced at 360 min.

Animal Model:

CBA/Ca (male, 16 weeks or older, 30-34 g)^[2]
Dosage:

16 mg/kg
Administration:

i.p.; administered 60 min before Efaroxan
Result:

Produced a significantly greater decrease in blood glucose than either compound alone.
No antagonism was observed; the combined effect was synergistic or at least additive.

Related Protocols :

Chemical Information

CAS. Nr. 189224-48-4
Appearance Solid
Molecular Weight 214.26
Formel C₁₃H₁₄N₂O
Color White to off-white
SMILES

CCC1(C2=NC=CN2)OC3=CC=CC=C3C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (466.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

4.6672 mL

23.3361 mL

46.6723 mL

5 mM

0.9334 mL

4.6672 mL

9.3345 mL

10 mM

0.4667 mL

2.3336 mL

4.6672 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.

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 (11.67 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 (11.67 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 (11.67 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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (299 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Bleck C, et al. Essential role of the imidazoline moiety in the insulinotropic effect but not the KATP channel-blocking effect of imidazolines; a comparison of the effects of efaroxan and its imidazole analogue, KU14R. Diabetologia. 2005;48:2567-2575.

[2]. Mayer G, et al. Effects of the imidazoline ligands efaroxan and KU14R on blood glucose homeostasis in the mouse. European journal of pharmacology. 2002 Nov 01;454(1):95-102. [Content Brief]

[3]. Lin MH, et al. Investigation of morin-induced insulin secretion in cultured pancreatic cells. Clin Exp Pharmacol Physiol. 2017; 44: 1254-1262.

[4]. Chan SL, et al. Characterization of a KATP channel-independent pathway involved in potentiation of insulin secretion by efaroxan. Diabetes. 2001 Feb;50(2):340-7.

[5]. Chan SL, et al. Evidence that the ability of imidazoline compounds to stimulate insulin secretion is not due to interaction with sigma receptors. European journal of pharmacology. 1997 Apr 04;323(2-3):241-4.

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
DMSO	1 mM	4.6672 mL	23.3361 mL	46.6723 mL	116.6807 mL
	5 mM	0.9334 mL	4.6672 mL	9.3345 mL	23.3361 mL
	10 mM	0.4667 mL	2.3336 mL	4.6672 mL	11.6681 mL
	15 mM	0.3111 mL	1.5557 mL	3.1115 mL	7.7787 mL
	20 mM	0.2334 mL	1.1668 mL	2.3336 mL	5.8340 mL
	25 mM	0.1867 mL	0.9334 mL	1.8669 mL	4.6672 mL
	30 mM	0.1556 mL	0.7779 mL	1.5557 mL	3.8894 mL
	40 mM	0.1167 mL	0.5834 mL	1.1668 mL	2.9170 mL
	50 mM	0.0933 mL	0.4667 mL	0.9334 mL	2.3336 mL
	60 mM	0.0778 mL	0.3889 mL	0.7779 mL	1.9447 mL
	80 mM	0.0583 mL	0.2917 mL	0.5834 mL	1.4585 mL
	100 mM	0.0467 mL	0.2334 mL	0.4667 mL	1.1668 mL

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KU14R

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