V-0219 (V0219) is a PAM/Positive Allosteric Modulator of GLP-1 (Glucagon-Like Peptide-1) Receptor with antidiabetic and weight-loss activity. Has the potential for treating 'Diabesity'.

Physicochemical Properties

Molecular Formula	C20H25F3N4O2
Molecular Weight	410.433315038681
Exact Mass	410.193
CAS #	878453-71-5
Related CAS #	V-0219 hydrochloride;2922283-73-4;(R)-V-0219 hydrochloride;(S)-V-0219 hydrochloride;(R)-V-0219;(S)-V-0219
PubChem CID	6486002
Appearance	Light yellow to yellow ointment
LogP	3
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	5
Heavy Atom Count	29
Complexity	510
Defined Atom Stereocenter Count	0
InChi Key	VFQGZIAZHIRPPQ-UHFFFAOYSA-N
InChi Code	InChI=1S/C20H25F3N4O2/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
Chemical Name	4-((1-((3-(4-(trifluoromethyl)phenyl)-1,2,4-oxadiazol-5-yl)methyl)piperidin-3-yl)methyl)morpholine
Synonyms	V0219 V-0219 V 0219
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
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

References

:J Med Chem. 2022 Apr 14;65(7):5449-5461.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~243.65 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (5.07 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 20.8 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: ≥ 2.08 mg/mL (5.07 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 20.8 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: ≥ 2.08 mg/mL (5.07 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 20.8 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	2.4365 mL	12.1823 mL	24.3647 mL
	5 mM	0.4873 mL	2.4365 mL	4.8729 mL
	10 mM	0.2436 mL	1.2182 mL	2.4365 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.