1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. VU0071063

VU0071063 

Cat. No.: HY-124424 Purity: 99.41%
Handling Instructions

VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC50=7.44 μM) 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.

For research use only. We do not sell to patients.

VU0071063 Chemical Structure

VU0071063 Chemical Structure

CAS No. : 333415-38-6

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Based on 1 publication(s) in Google Scholar

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Description

VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC50=7.44 μM) 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].

IC50 & Target

EC50: 7.44 μM (Kir6.2/SUR1)[1]

In Vitro

VU0071063 (1 nM~1 mM; HEK-293 cells) dose dependently opened 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

VU0071063 (50 mg/kg; i.p.; 4 hours) leads to a significant increase in blood glucose at 60 minutes[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

326.39

Formula

C₁₈H₂₂N₄O₂

CAS No.
SMILES

O=C(N1C)N(C)C2=C(N(CC3=CC=C(C(C)(C)C)C=C3)C=N2)C1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

References
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Keywords:

VU0071063VU 0071063VU-0071063Potassium ChannelKcsAPotentSpecificInsulinHyperpolarizationB-cellBlood-brain-barrierAlzheimerInhibitorinhibitorinhibit

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VU0071063
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