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Y-26763

Cat. No. M7498
Y-26763 Structure
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Biological Activity

Y-26763 is a kir6 (KATP) channel opener and active metabolite of Y-27152. Relaxes contracted rat aortic rings (IC50 = 0.027 mM) and inhibits glucose-induced insulin secretion in isolated human pancreatic β-cells in vitro. Produces hypotension in spontaneously hypertensive rats and displays cardioprotective properties in dogs following systemic administration in vivo.

Chemical Information
Molecular Weight 276.29
Formula C14H16N2O4
CAS Number 127408-31-5
Solubility (25°C) 1eq. NaOH 27.63 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] Kennett, et al. Neuropharmacology. Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated.

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