V-0219 hydrochloride
Based on 1 Customer Validation
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.
- Purity: 99.39%
- CAS No.: 2922283-73-4
- Formula: C20H26ClF3N4O2
- Molecular Weight:446.89
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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GLP-1 |
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.
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Cell Line:rat INS-1 insulinoma β-cells
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Concentration:0.01, 0.1, 1 nM
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Incubation Time:30 min
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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.
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.
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Animal Model:C57BL/6N (male, wild-type)[1]
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Dosage:0.1 mg/kg
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Administration:i.p.; single dose 30 minutes prior to glucose load
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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.
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Animal Model:Wistar Rats (male, 400 g)[1]
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Dosage:1 μg/kg
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Administration:i.c.v.; single dose
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Result:Potentiated Exendin-4-induced feeding inhibition.
Decreased the IC50 of Exendin-4's feeding inhibitory effect from 394 ng to 89 ng.
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Animal Model:Wistar Rats (male, 400 g)[1]
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Dosage:1 mg/kg
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Administration:i.p.; single dose 30 minutes prior to glucose load
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Result:Reduced the time spent in hyperglycemia after glucose load compared to vehicle control.
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Animal Model:fatty Zucker (fa/fa) Rats (male, 12-16 weeks, 380-450 g)[1]
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Dosage:0.1; 2 mg/kg
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Administration:i.p.; single dose 30 minutes prior to glucose load
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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.
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Animal Model:Wistar Rats (male, 400 g)[1]
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Dosage:0.5; 1 mg/kg
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Administration:i.p.; single dose
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Result:Caused no significant changes in time spent in closed arms or total arm entries compared to vehicle control.
Chemical Information
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CAS No. 2922283-73-4
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Appearance Solid
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Molecular Weight 446.89
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Formula C20H26ClF3N4O2
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Color White to off-white
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SMILES
FC(C1=CC=C(C2=NOC(CN3CC(CN4CCOCC4)CCC3)=N2)C=C1)(F)F.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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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
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (277 KB)
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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)
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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 (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 | 2.2377 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 |
V-0219 hydrochloride Related Classifications
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