V-0219 hydrochloride

Name: V-0219 hydrochloride
Brand: MedChemExpress
SKU: HY-143312A
Rating: 4.5 (1 reviews)

Cat. No.: HY-143312A Purity: 99.39%: Data Sheet
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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.

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

V-0219 hydrochloride Chemical Structure

CAS No. : 2922283-73-4

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of V-0219 hydrochloride:

(R)-V-0219 hydrochloride In-stock
(S)-V-0219 hydrochloride In-stock
V-0219 In-stock
(R)-V-0219 Get quote
(S)-V-0219 Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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	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.

Molecular Weight

446.89

Formula

C₂₀H₂₆ClF₃N₄O₂

CAS No.

2922283-73-4

Appearance

Solid

Color

White to off-white

SMILES

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

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 (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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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)

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 (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.
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 (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.
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 (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

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 (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

Purity: 99.39%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (249 KB) HNMR (252 KB) LCMS (339 KB)

Handling Instructions (2659 KB)

References

[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]

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