V-0219 HCl (Compound 9) is an orally bioactive glucagon-like peptide-1 receptor (GLP-1R) PAM (positive allosteric modulator). V-0219 HCl may be utilized in studies of obesity-related diabetes.

Physicochemical Properties

Molecular Formula	C20H26CLF3N4O2
Molecular Weight	446.894254207611
Exact Mass	446.169
CAS #	2922283-73-4
Related CAS #	V-0219;878453-71-5;(R)-V-0219 hydrochloride;(S)-V-0219 hydrochloride;(R)-V-0219;(S)-V-0219
PubChem CID	166604052
Appearance	White to off-white solid powder
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	5
Heavy Atom Count	30
Complexity	510
Defined Atom Stereocenter Count	0
InChi Key	PTRIYHLSBQMDQM-UHFFFAOYSA-N
InChi Code	InChI=1S/C20H25F3N4O2.ClH/c21-20(22,23)17-5-3-16(4-6-17)19-24-18(29-25-19)14-27-7-1-2-15(13-27)12-26-8-10-28-11-9-26;/h3-6,15H,1-2,7-14H2;1H
Chemical Name	4-[[1-[[3-[4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]methyl]piperidin-3-yl]methyl]morpholine;hydrochloride
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	GLP-1R[1]
References	[1]. 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.

Solubility Data

Solubility (In Vitro)

DMSO: 100 mg/mL (223.77 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.