| Identification | Back Directory | [Name]
7-(4-TERT-BUTYLBENZYL)-1,3-DIMETHYL-3,7-DIHYDRO-1H-PURINE-2,6-DIONE | [CAS]
333415-38-6 | [Synonyms]
VU0071063
TOSLAB 808036
7-(4-(tert-butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione
7-(4-TERT-BUTYLBENZYL)-1,3-DIMETHYL-3,7-DIHYDRO-1H-PURINE-2,6-DIONE
7-[[4-(1,1-Dimethylethyl)phenyl]methyl]-3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione
1H-Purine-2,6-dione, 7-[[4-(1,1-dimethylethyl)phenyl]methyl]-3,7-dihydro-1,3-dimethyl- | [Molecular Formula]
C18H22N4O2 | [MDL Number]
MFCD02648040 | [MOL File]
333415-38-6.mol | [Molecular Weight]
326.39 |
| Hazard Information | Back Directory | [Description]
VU0071063 is a potent and selective activator of the inward-rectifier potassium channel (Kir) 6.2 and sulfonylurea receptor (SUR) 1 (EC50 = 7 μM using whole cell patch clamp electrophysiology). It is selective for SUR1-containing Kir6.1 or Kir6.2 channels over SUR2A, Kir2.1, Kir2.2, Kir2.3, Kir3.1/3/2, and voltage-gated potassium channel 2.1. VU0071063 inhibits glucose-stimulated calcium entry in isolated mouse pancreatic β-cells. | [Uses]
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]. | [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)[1] | | Dosage: | 50 mg/kg (Pharmacokinetic analysis) | | Administration: | I.p. | | Result: | Led to a significant increase in blood glucose at 60 minutes. |
| [storage]
Store at -20°C | [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. DOI:10.1124/jpet.119.257204
[2] Raphemot R, et al. Direct activation of β-cell KATP channels with a novel xanthine derivative. Mol Pharmacol. 2014;85(6):858-865. DOI:10.1124/mol.114.091884 |
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