VU0071063

Name: VU0071063
Brand: MedChemExpress
SKU: HY-124424
Rating: 4.5 (1 reviews)

Cat. No.: HY-124424 Purity: 99.71%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

VU0071063 Chemical Structure

CAS No. : 333415-38-6

Size	Price	Stock	Quantity
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

IC₅₀ & 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].

MedChemExpress (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].

MedChemExpress (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)^[1]
Dosage:	50 mg/kg (Pharmacokinetic analysis)
Administration:	I.p.
Result:	Led to a significant increase in blood glucose at 60 minutes.

Molecular Weight

326.39

Formula

C₁₈H₂₂N₄O₂

CAS No.

333415-38-6

Appearance

Solid

Color

White to off-white

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)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (306.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.0638 mL	15.3191 mL	30.6382 mL
5 mM	0.6128 mL	3.0638 mL	6.1276 mL
10 mM	0.3064 mL	1.5319 mL	3.0638 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.71%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (250 KB) HNMR (242 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

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

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0638 mL	15.3191 mL	30.6382 mL	76.5955 mL
	5 mM	0.6128 mL	3.0638 mL	6.1276 mL	15.3191 mL
	10 mM	0.3064 mL	1.5319 mL	3.0638 mL	7.6595 mL
	15 mM	0.2043 mL	1.0213 mL	2.0425 mL	5.1064 mL
	20 mM	0.1532 mL	0.7660 mL	1.5319 mL	3.8298 mL
	25 mM	0.1226 mL	0.6128 mL	1.2255 mL	3.0638 mL
	30 mM	0.1021 mL	0.5106 mL	1.0213 mL	2.5532 mL
	40 mM	0.0766 mL	0.3830 mL	0.7660 mL	1.9149 mL
	50 mM	0.0613 mL	0.3064 mL	0.6128 mL	1.5319 mL
	60 mM	0.0511 mL	0.2553 mL	0.5106 mL	1.2766 mL
	80 mM	0.0383 mL	0.1915 mL	0.3830 mL	0.9574 mL
	100 mM	0.0306 mL	0.1532 mL	0.3064 mL	0.7660 mL

VU0071063 Related Classifications

Neurological Disease Others

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VU0071063333415-38-6VU 0071063VU-0071063Potassium ChannelKcsAPotentSpecificInsulinHyperpolarizationB-cellBlood-brain-barrierAlzheimerInhibitorinhibitorinhibit

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VU0071063

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Complete Stock Solution Preparation Table

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