333415-38-6

333415-38-6 structure

Name: VU0071063
Chemical Name: 7-(4-tert-Butyl-benzyl)-1,3-dimethyl-3,7-dihydro-purine-2,6-dione
CAS Number: 333415-38-6
Molecular Formula: C₁₈H₂₂N₄O₂
Molecular Weight: 326.393
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
Create Date: 2018-07-12 08:57:38
Modify Date: 2024-04-03 11:26:44
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].

Name	7-(4-tert-Butyl-benzyl)-1,3-dimethyl-3,7-dihydro-purine-2,6-dione
Synonyms	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

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.

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

RIDADR	NONH for all modes of transport

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