Midaglizole ((±)-DG5128 free base, DG5128 free base) is a potent α2-adrenoceptor antagonist. Midaglizole is a blood sugar-lowering drug. Midaglizole increases blood pressure and lowers blood sugar levels.

Physicochemical Properties

Molecular Formula	C16H17N3
Molecular Weight	251.33
Exact Mass	251.142
CAS #	66529-17-7
Related CAS #	Midaglizole hydrochloride;79689-25-1
PubChem CID	68864
Appearance	White to off-white solid powder
Density	1.14g/cm3
Boiling Point	460ºC at 760 mmHg
Flash Point	232ºC
Index of Refraction	1.629
LogP	2.369
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	2
Rotatable Bond Count	4
Heavy Atom Count	19
Complexity	307
Defined Atom Stereocenter Count	0
SMILES	C1CN=C(N1)CC(C2=CC=CC=C2)C3=CC=CC=N3
InChi Key	TYZQFNOLWJGHRZ-UHFFFAOYSA-N
InChi Code	InChI=1S/C16H17N3/c1-2-6-13(7-3-1)14(12-16-18-10-11-19-16)15-8-4-5-9-17-15/h1-9,14H,10-12H2,(H,18,19)
Chemical Name	2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-phenylethyl]pyridine
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

ln Vitro	With EC50 values of 200 nM and 24 µM for rat islets and the MIN6 β-cell line, respectively, midaglizole promotes the release of insulin[3].
ln Vivo	In rats, midaglizole (3, 30 mg/kg; IV) raises blood pressure[1]. Dags' blood glucose levels are lowered with midaglizole (0.2, 1, 2 mg/kg; infusion)[2].
Animal Protocol	Animal/Disease Models: 290-450 g , Male Wistar rats[1] Doses: 3, 30 mg/kg Route of Administration: Iv Experimental Results: Increased the blood pressure by 27 and 64 mmHg at 3, 30 mg/kg, respectively. Animal/Disease Models: Dogs[2] Doses: 0.2, 1, 2 mg/kg Route of Administration: Superior pancreaticoduodeneal artery infusion Experimental Results: decreased blood glucose levels by stimulating insulin release from the pancreatic islets.
References	[1]. Hirohashi M, et al. Intrinsic pressor activity of midaglizole, an alpha-2 adrenoceptor antagonist, in pithed rats. Jpn J Pharmacol. 1990 Aug;53(4):519-20. [2]. Ohneda K, et al. Mechanism of insulin secretion by midaglizole. Diabetes Res Clin Pract. 1993 Feb;19(2):127-32. [3]. Proks P, et al. Inhibition of recombinant K(ATP) channels by the antidiabetic agents midaglizole, LY397364 and LY389382. Eur J Pharmacol. 2002 Sep 27;452(1):11-9.

Solubility Data

Solubility (In Vitro)

DMSO: 162.5 mg/mL (646.56 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 16.25 mg/mL (64.66 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 162.5 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: ≥ 16.25 mg/mL (64.66 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 162.5 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: ≥ 16.25 mg/mL (64.66 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 162.5 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	3.9788 mL	19.8942 mL	39.7883 mL
	5 mM	0.7958 mL	3.9788 mL	7.9577 mL
	10 mM	0.3979 mL	1.9894 mL	3.9788 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.