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KU14R

Cat. No. M3734
KU14R Structure
Size Price Availability Quantity
10mg USD 105  USD105 In stock
50mg USD 410  USD410 In stock
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Quality Control & Documentation
Biological Activity

KU14R has been shown to block the effects of the atypical I(3) agonist efaroxan at the level of the ATP-sensitive K(+) (K(ATP)) channel in isolated pancreatic islet beta cells, but its effects in vivo are not known. KU14R does not act as an antagonist of either efaroxan or S22068 at an imidazoline site in vivo.KU-14R, an I(3)-R antagonist, partially attenuated responses to IAA-RP.

Chemical Information
Molecular Weight 214.26
Formula C13H14N2O
CAS Number 189224-48-4
Solubility (25°C) DMSO 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Bozdagi O, et al. J Neurophysiol. Imidazoleacetic acid-ribotide induces depression of synaptic responses in hippocampus through activation of imidazoline receptors.

[2] Bleck C, et al. Diabetologia. 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.

[3] Mayer G, et al. Eur J Pharmacol. Effects of the imidazoline ligands efaroxan and KU14R on blood glucose homeostasis in the mouse.

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