Enavogliflozin (DWP-16001), an antidiabetic active molecule, is an orally bioactive, first-in-class, selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor.

Physicochemical Properties

Molecular Formula	C24H27CLO6
Molecular Weight	446.92
Exact Mass	446.149
CAS #	1415472-28-4
PubChem CID	71076840
Appearance	White to off-white solid powder
Density	1.4±0.1 g/cm3
Boiling Point	666.1±55.0 °C at 760 mmHg
Flash Point	356.7±31.5 °C
Vapour Pressure	0.0±2.1 mmHg at 25°C
Index of Refraction	1.666
LogP	4.9
Hydrogen Bond Donor Count	4
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	5
Heavy Atom Count	31
Complexity	609
Defined Atom Stereocenter Count	5
SMILES	C1CC1C2=CC=C(C=C2)CC3=CC(=C4CCOC4=C3Cl)[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)CO)O)O)O
InChi Key	KORCWPOBTZTAFI-YVTYUBGGSA-N
InChi Code	InChI=1S/C24H27ClO6/c25-19-15(9-12-1-3-13(4-2-12)14-5-6-14)10-17(16-7-8-30-23(16)19)24-22(29)21(28)20(27)18(11-26)31-24/h1-4,10,14,18,20-22,24,26-29H,5-9,11H2/t18-,20-,21+,22-,24+/m1/s1
Chemical Name	(2S,3R,4R,5S,6R)-2-[7-chloro-6-[(4-cyclopropylphenyl)methyl]-2,3-dihydro-1-benzofuran-4-yl]-6-(hydroxymethyl)oxane-3,4,5-triol
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

Targets	SGLT2
ln Vitro	The antidiabetic medication enavogliflozin (DWP-16001) is an oral, potent, highly selective, and best-in-class sodium-glucose cotransporter-2 (SGLT-2) inhibitor[1][2][3].
References	[1]. Daewoong speeds up developing antidiabetic Enavogliflozin. [2]. These are the results of clinical trials of the diabetes drug Enavogliflozin and Metformin. [3]. Global Diabetes Pipeline Landscape Report 2020 Featuring Daewoong's Enavogliflozin & Janssen Biotech's Golimumab Among Others - ResearchAndMarkets.com.

Solubility Data

Solubility (In Vitro)

DMSO: 100 mg/mL (223.75 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	2.2375 mL	11.1877 mL	22.3754 mL
	5 mM	0.4475 mL	2.2375 mL	4.4751 mL
	10 mM	0.2238 mL	1.1188 mL	2.2375 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.