Glucagon receptor blocker (antagonist)s-1 is a highly active glucagon receptor blocker (antagonist).

Physicochemical Properties

Molecular Formula	C29H34FNO2
Molecular Weight	447.58416
Exact Mass	447.257
CAS #	503559-84-0
PubChem CID	66576985
Appearance	White to off-white solid powder
Density	1.094
LogP	7.799
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	8
Heavy Atom Count	33
Complexity	602
Defined Atom Stereocenter Count	0
SMILES	FC1=CC=C(C2=C(/C=C/C)C(C(C)C)=NC(C(C)C)=C2C(C)O)C(OCC3=CC=CC=C3)=C1
InChi Key	HERVQUFQZXZOBU-YRNVUSSQSA-N
InChi Code	InChI=1S/C29H34FNO2/c1-7-11-24-27(26(20(6)32)29(19(4)5)31-28(24)18(2)3)23-15-14-22(30)16-25(23)33-17-21-12-9-8-10-13-21/h7-16,18-20,32H,17H2,1-6H3/b11-7+
Chemical Name	1-[4-(4-fluoro-2-phenylmethoxyphenyl)-2,6-di(propan-2-yl)-5-[(E)-prop-1-enyl]pyridin-3-yl]ethanol
Synonyms	Glucagon receptor antagonists-1
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: ~50 mg/mL (~111.7 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.75 mg/mL (6.14 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 27.5 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: ≥ 2.75 mg/mL (6.14 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 27.5 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	2.2342 mL	11.1712 mL	22.3424 mL
	5 mM	0.4468 mL	2.2342 mL	4.4685 mL
	10 mM	0.2234 mL	1.1171 mL	2.2342 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.