Glucagon receptor blocker (antagonist)s-2 is a highly active glucagon receptor blocker (antagonist).

Physicochemical Properties

Molecular Formula	C22H30FNO2
Molecular Weight	359.48
Exact Mass	361.24
CAS #	202917-18-8
Related CAS #	Glucagon receptor antagonists-3; 202917-17-7
PubChem CID	77147236
Appearance	Solid powder
Density	1.085
Boiling Point	469.6ºC at 760 mmHg
Flash Point	237.8ºC
LogP	5.548
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	6
Heavy Atom Count	26
Complexity	552
Defined Atom Stereocenter Count	0
InChi Key	OINVVPOIGFSNHM-VLIAUNLRSA-N
InChi Code	InChI=1S/C22H32FNO2/c1-7-8-17-20(16-10-9-15(23)11-18(16)26)19(14(6)25)22(13(4)5)24-21(17)12(2)3/h9-14,20,24-26H,7-8H2,1-6H3/t14-,20+/m1/s1
Chemical Name	5-fluoro-2-[(4S)-3-[(1R)-1-hydroxyethyl]-2,6-di(propan-2-yl)-5-propyl-1,4-dihydropyridin-4-yl]phenol
Synonyms	Glucagon receptor antagonists-2
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

[1]. Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists. Bioorganic & Medicinal Chemistry Letters (2002), 12(23), 3421-3424.

Solubility Data

Solubility (In Vitro)

DMSO: ~16.7 mg/mL (~46.4 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 1.67 mg/mL (4.65 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 16.7 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: ≥ 1.67 mg/mL (4.65 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 16.7 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	2.7818 mL	13.9090 mL	27.8180 mL
	5 mM	0.5564 mL	2.7818 mL	5.5636 mL
	10 mM	0.2782 mL	1.3909 mL	2.7818 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.