2. GPCR/G Protein
  3. GLP Receptor
  4. V-0219

V-0219 is an orally active glucagon-like peptide-1 receptor (GLP-1R) positive allosteric modulator. V-0219 potentiates GLP-1R stimulation, and enhances GLP-1-induced cAMP production and insulin secretion. V-0219 potentiates glucose-dependent insulin secretion. V-0219 improves glucose handling in normal and diabetic rodents. V-0219 can be used for the research of obesity-associated diabetes.

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V-0219

V-0219 Chemical Structure

CAS No. : 878453-71-5

Size Price Stock Quantity
Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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25 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of V-0219:

V-0219 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

V-0219 is an orally active glucagon-like peptide-1 receptor (GLP-1R) positive allosteric modulator. V-0219 potentiates GLP-1R stimulation, and enhances GLP-1-induced cAMP production and insulin secretion. V-0219 potentiates glucose-dependent insulin secretion. V-0219 improves glucose handling in normal and diabetic rodents. V-0219 can be used for the research of obesity-associated diabetes[1].

IC50 & Target[1]

GLP-1

 

In Vitro

V-0219 (compound 9) (0.001-1 nM; 15 min) potently potentiates GLP-1-stimulated cAMP accumulation in HEK-293 cells expressing human GLP-1R[1].
V-0219 (0.01-1 nM; 30 min) potentiates GLP-1-induced insulin secretion in rat INS-1 β-cells, and this effect is mediated by the GLP-1R[1].

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

V-0219 Related Antibodies

ELISA Assay[1]

Cell Line: rat INS-1 insulinoma β-cells
Concentration: 0.01, 0.1, 1 nM
Incubation Time: 30 min
Result: Produced an 1.8-fold potentiation of GLP-1-induced insulin secretion at 0.1 nM, with an EC50 of 0.25 nM.
Reached a maximal response plateau at 0.1 nM when combined with a fixed 0.2 nM GLP-1, with an EC50 of 0.008 nM.
Parmacokinetics
Species Dose Route Tmax Cmax AUC0-t AUC0-inf T1/2 F C0 CL Vss
Rat[1] 2 mg/kg i.v. / / 277.61 ng·h/mL 310.92 ng·h/mL 3.25 h / 491.99 ng/mL 107.34 mL/min/kg 18.05 L/kg
Rat[1] 10 mg/kg p.o. 0.83 h 184.91 ng/mL 540.25 ng·h/mL 644.45 ng·h/mL 2.86 h 38.92 % / / /
In Vivo

V-0219 (compound 9) (0.1 mg/kg; i.p.; single dose 30 minutes prior to glucose load) improves glucose handling in wild-type mice via GLP-1R-mediated activity[1].
V-0219 (1 μg/kg; i.c.v.; single dose) potentiates Exendin-4 (HY-13443)-induced feeding inhibition in rats[1].
V-0219 (1 mg/kg; i.p.; single dose 30 minutes prior to glucose load) improves glucose handling in normal Wistar rats by reducing hyperglycemia duration[1].
V-0219 (0.1 and 2 mg/kg; i.p.; single dose 30 minutes prior to glucose load) improves glucose handling in diabetic fatty Zucker rats via enhancement of first-phase insulin secretion[1].
V-0219 (0.5-1 mg/kg; i.p.; single dose) does not induce anxiety-like behavior in Wistar rats[1].

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

Animal Model: C57BL/6N (male, wild-type)[1]
Dosage: 0.1 mg/kg
Administration: i.p.; single dose 30 minutes prior to glucose load
Result: Lowered post-load plasma glucose levels compared to vehicle control.
Showed no glucose-lowering effect in GLP-1R knockout mice at the same dose.
Animal Model: Wistar Rats (male, 400 g)[1]
Dosage: 1 μg/kg
Administration: i.c.v.; single dose
Result: Potentiated Exendin-4-induced feeding inhibition.
Decreased the IC50 of Exendin-4's feeding inhibitory effect from 394 ng to 89 ng.
Animal Model: Wistar Rats (male, 400 g)[1]
Dosage: 1 mg/kg
Administration: i.p.; single dose 30 minutes prior to glucose load
Result: Reduced the time spent in hyperglycemia after glucose load compared to vehicle control.
Animal Model: fatty Zucker (fa/fa) Rats (male, 12-16 weeks, 380-450 g)[1]
Dosage: 0.1; 2 mg/kg
Administration: i.p.; single dose 30 minutes prior to glucose load
Result: Improved glucose handling, with the effect occurring during the first phase of insulin secretion promoted by the glucose load.
Showed no improvement at a 0.1 mg/kg dose.
Animal Model: Wistar Rats (male, 400 g)[1]
Dosage: 0.5; 1 mg/kg
Administration: i.p.; single dose
Result: Caused no significant changes in time spent in closed arms or total arm entries compared to vehicle control.
Molecular Weight

410.43

Formula

C20H25F3N4O2
CAS No.
Appearance

Solid-Liquid Mixture

Color

Light yellow to yellow

SMILES

FC(C1=CC=C(C2=NOC(CN3CC(CN4CCOCC4)CCC3)=N2)C=C1)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (243.65 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 2.4365 mL 12.1823 mL 24.3647 mL
5 mM 0.4873 mL 2.4365 mL 4.8729 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. 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: ≥ 2.08 mg/mL (5.07 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.07 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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).
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: 99.90%

SDS (252 KB)

COA (247 KB) HNMR (225 KB) RP-HPLC (262 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
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. 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 2.4365 mL 12.1823 mL 24.3647 mL 60.9117 mL
5 mM 0.4873 mL 2.4365 mL 4.8729 mL 12.1823 mL
10 mM 0.2436 mL 1.2182 mL 2.4365 mL 6.0912 mL
15 mM 0.1624 mL 0.8122 mL 1.6243 mL 4.0608 mL
20 mM 0.1218 mL 0.6091 mL 1.2182 mL 3.0456 mL
25 mM 0.0975 mL 0.4873 mL 0.9746 mL 2.4365 mL
30 mM 0.0812 mL 0.4061 mL 0.8122 mL 2.0304 mL
40 mM 0.0609 mL 0.3046 mL 0.6091 mL 1.5228 mL
50 mM 0.0487 mL 0.2436 mL 0.4873 mL 1.2182 mL
60 mM 0.0406 mL 0.2030 mL 0.4061 mL 1.0152 mL
80 mM 0.0305 mL 0.1523 mL 0.3046 mL 0.7614 mL
100 mM 0.0244 mL 0.1218 mL 0.2436 mL 0.6091 mL
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V-0219 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:

V-0219878453-71-5V0219V 0219GLP Receptorexendin-4cAMPdiabetic fatty Zucker ratsrat INS-1 β-cellshuman EndoC-βH1 pancreatic cellsglucagon-like peptide-1 receptorWistar ratsinsulin secretionHEK-293 cellsGLP-1RInhibitorinhibitorinhibit

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