VU0071063

Names

[ Name ]:
VU0071063

[Synonym ]:
1H-Purine-2,6-dione, 7-[[4-(1,1-dimethylethyl)phenyl]methyl]-3,7-dihydro-1,3-dimethyl-
MFCD02648040
1H-Purine-2,6-dione, 3,7-dihydro-7-(4-tert-butylbenzyl)-1,3-dimethyl-
7-(4-tert-Butyl-benzyl)-1,3-dimethyl-3,7-dihydro-purine-2,6-dione
1,3-Dimethyl-7-[4-(2-methyl-2-propanyl)benzyl]-3,7-dihydro-1H-purine-2,6-dione

Biological Activity

[Description]:

VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC50=7.44 μM) and can be used for investigating Kir6.2/SUR1 expressed in the pancreas and brain. VU0071063 inhibits insulin secretion by inducing hyperpolarization of β-cell membrane potential. VU0071063 chemotype has a very steep structure-activity relationships[1][2].

[Related Catalog]:

Research Areas >> Others

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[Target]

EC50: 7.44 μM (Kir6.2/SUR1)[1]

[In Vitro]

VU0071063 (1 nM~1 mM; HEK-293 cells) dose dependently opens Kir6.2/SUR1. VU0071063 (0~20 μM; isolated cells) inhibits β-Cell excitability in mouse Islets. VU0071063 (10 μM; 1 hour; isolated cells) inhibits glucose-stimulated insulin secretion[1]. VU0071063 dose dependently and reversibly hyperpolarizes the β-cell membrane potential, which, in turn, inhibits glucose-stimulated Ca2+ entry and insulin secretion. The actions of VU0071063 on the β-cell membrane potential are reversed by tolbutamide, and glucose stimulated insulin secretion is unaffected by the inactive analog 34MT, indicating that the effects are mediated through Kir6.2/SUR1[1].

[In Vivo]

VU0071063 (50 mg/kg; i.p.; 4 hours) leads to a significant increase in blood glucose at 60 minutes[1]. Animal Model: Male C57BL/6 mice (10–12 weeks age) Dosage: 50 mg/kg (Pharmacokinetic analysis) Administration: I.p.; 4 hours Result: led to a significant increase in blood glucose at 60 minutes.

[References]

[1]. Kharade SV, et al. Structure-Activity Relationships, Pharmacokinetics, and Pharmacodynamics of the Kir6.2/SUR1-Specific Channel Opener VU0071063. J Pharmacol Exp Ther. 2019;370(3):350-359.

[2]. Raphemot R, et al. Direct activation of β-cell KATP channels with a novel xanthine derivative. Mol Pharmacol. 2014;85(6):858-865.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
507.8±42.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₈H₂₂N₄O₂

[ Molecular Weight ]:
326.393

[ Flash Point ]:
260.9±27.9 °C

[ Exact Mass ]:
326.174286

[ LogP ]:
3.23

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.615

[ Storage condition ]:
2-8°C

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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