Art. -Nr.: HY-143312A

V-0219 hydrochloride

Name: V-0219 hydrochloride
Brand: MedChemExpress
SKU: HY-143312A
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V-0219 hydrochloride is an orally active glucagon-like peptide-1 receptor (GLP-1R) positive allosteric modulator. V-0219 hydrochloride potentiates GLP-1R stimulation, and enhances GLP-1-induced cAMP production and insulin secretion. V-0219 hydrochloride potentiates glucose-dependent insulin secretion. V-0219 hydrochloride improves glucose handling in normal and diabetic rodents. V-0219 hydrochloride can be used for the research of obesity-associated diabetes.

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Reinheit : 99.39%
CAS. Nr.: 2922283-73-4
Formel: C₂₀H₂₆ClF₃N₄O₂
Molecular Weight:446.89

Speicherung:

4°C, sealed storage, away from moisture

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

V-0219 hydrochloride Chemical Structure

CAS. Nr.: 2922283-73-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (3)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

GLP-1

In Vitro

V-0219 (compound 9) (0.001-1 nM; 15 min) hydrochloride potently potentiates GLP-1-stimulated cAMP accumulation in HEK-293 cells expressing human GLP-1R^[1].
V-0219 (0.01-1 nM; 30 min) hydrochloride 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. Further protocols information, click here.

ELISA Assay^[1]

View Protocol

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	AUC_0-t	AUC_0-inf	T_1/2	F	T_max	C_max	C₀	CL
Rat^[1]	10 mg/kg	p.o.	540.25 ng·h/mL	644.45 ng·h/mL	2.86 h	38.92 %	0.83 h	184.91 ng/mL	/	/
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

In Vivo

V-0219 (compound 9) (0.1 mg/kg; i.p.; single dose 30 minutes prior to glucose load) hydrochloride improves glucose handling in wild-type mice via GLP-1R-mediated activity^[1].
V-0219 (1 μg/kg; i.c.v.; single dose) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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.

Chemical Information

CAS. Nr. 2922283-73-4
Appearance Solid
Molecular Weight 446.89
Formel C₂₀H₂₆ClF₃N₄O₂
Color White to off-white
SMILES

FC(C1=CC=C(C2=NOC(CN3CC(CN4CCOCC4)CCC3)=N2)C=C1)(F)F.[H]Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (223.77 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2377 mL

11.1884 mL

22.3769 mL

5 mM

0.4475 mL

2.2377 mL

4.4754 mL

10 mM

0.2238 mL

1.1188 mL

2.2377 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (5.59 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.59 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.59 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

All Signal Pathway Related Cell Biology

Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Human Islet Cell Culture
The method of preserving islets in vitro, with purified reduced immunogenicity. The steps are islet isolation, islet cell purification, in vitro determination of islet function and islet cell culture.
Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Decara JM, et al. Discovery of V-0219: A Small-Molecule Positive Allosteric Modulator of the Glucagon-Like Peptide-1 Receptor toward Oral Treatment for "Diabesity". J Med Chem. 2022 Apr 14;65(7):5449-5461. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2377 mL	11.1884 mL	22.3769 mL	55.9422 mL
	5 mM	0.4475 mL	2.2377 mL	4.4754 mL	11.1884 mL
	10 mM	0.2238 mL	1.1188 mL	2.2377 mL	5.5942 mL
	15 mM	0.1492 mL	0.7459 mL	1.4918 mL	3.7295 mL
	20 mM	0.1119 mL	0.5594 mL	1.1188 mL	2.7971 mL
	25 mM	0.0895 mL	0.4475 mL	0.8951 mL	2.2377 mL
	30 mM	0.0746 mL	0.3729 mL	0.7459 mL	1.8647 mL
	40 mM	0.0559 mL	0.2797 mL	0.5594 mL	1.3986 mL
	50 mM	0.0448 mL	0.2238 mL	0.4475 mL	1.1188 mL
	60 mM	0.0373 mL	0.1865 mL	0.3729 mL	0.9324 mL
	80 mM	0.0280 mL	0.1399 mL	0.2797 mL	0.6993 mL
	100 mM	0.0224 mL	0.1119 mL	0.2238 mL	0.5594 mL

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V-0219 hydrochloride