2. GPCR/G Protein
  3. GCGR
  4. VU0453379

VU0453379 is a blood-brain barrier permeable GLP-1R positive allosteric modulator (PAM) with an EC50 value of 1.3 μM. VU0453379 potentiates the actions of endogenous GLP-1 and synthetic peptide agonists, and promotes GLP-1 receptor internalization. VU0453379 stimulates insulin secretion from primary mouse islets. VU0453379 enhances the function of endogenous GLP-1R and reverses catalepsy in animal models. VU0453379 is useful for research on Parkinson's disease and type 2 diabetes.

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

VU0453379

VU0453379 Chemical Structure

CAS No. : 1638646-27-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
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500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of VU0453379:

VU0453379 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

VU0453379 is a blood-brain barrier permeable GLP-1R positive allosteric modulator (PAM) with an EC50 value of 1.3 μM. VU0453379 potentiates the actions of endogenous GLP-1 and synthetic peptide agonists, and promotes GLP-1 receptor internalization. VU0453379 stimulates insulin secretion from primary mouse islets. VU0453379 enhances the function of endogenous GLP-1R and reverses catalepsy in animal models. VU0453379 is useful for research on Parkinson's disease and type 2 diabetes[1].

IC50 & Target

EC50: 1.3 μM (GLP-1R)[1]
In Vitro

VU0453379 (1.3-30 μM) potentiates native GLP-1, exenatide, and liraglutide in human GLP-1R 9-3-H cells with EC50 values ranging from 1.8 μM to 30 μM, acts as an ago-PAM alone, and enhances GLP-1 receptor internalization without significant β-arrestin recruitment effects[1].

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

VU0453379 Related Antibodies
Parmacokinetics
Species Dose Route CL T1/2 Vss F
Rat[1] 1 mg/kg p.o. 72 mL/min/kg 58 min 4.0 L/kg <1 %
In Vivo

VU0453379 (10-30 mg/kg; i.p.; single administration) dose-dependently reverses haloperidol (HY-14538)-induced catalepsy in rats[1].

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

Animal Model: Sprague-Dawley (male; 10-12 per treatment group; Haloperidol-induced catalepsy model)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: i.p.; single dose
Result: Produced a 36.3% reversal of catalepsy in rats challenged with 0.75 mg/kg Haloperidol.
Produced a 50.4% reversal of catalepsy in rats challenged with 0.75 mg/kg Haloperidol.
Produced a 36.6% reversal of catalepsy in rats challenged with 1.5 mg/kg Haloperidol.
Reduced latency to withdraw forepaws from a horizontal bar relative to vehicle controls with statistical significance.
Molecular Weight

434.57

Formula

C26H34N4O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC[C@H]1N(CCC1)C(C)C)C(C2=C3N(C4=C2C=CC=C4)C)=CN(C3=O)C5CCCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (230.11 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 2.3011 mL 11.5056 mL 23.0113 mL
5 mM 0.4602 mL 2.3011 mL 4.6023 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 (sealed storage, away from moisture). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (5.75 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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 (sealed storage, away from moisture)

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
References

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3011 mL 11.5056 mL 23.0113 mL 57.5281 mL
5 mM 0.4602 mL 2.3011 mL 4.6023 mL 11.5056 mL
10 mM 0.2301 mL 1.1506 mL 2.3011 mL 5.7528 mL
15 mM 0.1534 mL 0.7670 mL 1.5341 mL 3.8352 mL
20 mM 0.1151 mL 0.5753 mL 1.1506 mL 2.8764 mL
25 mM 0.0920 mL 0.4602 mL 0.9205 mL 2.3011 mL
30 mM 0.0767 mL 0.3835 mL 0.7670 mL 1.9176 mL
40 mM 0.0575 mL 0.2876 mL 0.5753 mL 1.4382 mL
50 mM 0.0460 mL 0.2301 mL 0.4602 mL 1.1506 mL
60 mM 0.0384 mL 0.1918 mL 0.3835 mL 0.9588 mL
80 mM 0.0288 mL 0.1438 mL 0.2876 mL 0.7191 mL
100 mM 0.0230 mL 0.1151 mL 0.2301 mL 0.5753 mL
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VU0453379 Related Classifications

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:

VU04533791638646-27-1VU 0453379VU-0453379GCGRGlucagon ReceptorGLP-1R positive allosteric modulatorParkinson's diseasetype 2 diabetesSprague-DawleyratInhibitorinhibitorinhibit

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