HFI-142 is an insulin-regulated aminopeptidase (IRAP) inhibitor (antagonist) with Ki of 2.01 μM.

Physicochemical Properties

Molecular Formula	C17H16N2O4
Molecular Weight	312.319944381714
Exact Mass	312.111
CAS #	332164-34-8
PubChem CID	655457
Appearance	White to off-white solid powder
LogP	2.4
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	4
Heavy Atom Count	23
Complexity	479
Defined Atom Stereocenter Count	0
SMILES	CCOC(C1=C(N)OC2=CC(=CC=C2C1C1=CC=CN=C1)O)=O
InChi Key	JOPNHSIHFSZJMB-UHFFFAOYSA-N
InChi Code	InChI=1S/C17H16N2O4/c1-2-22-17(21)15-14(10-4-3-7-19-9-10)12-6-5-11(20)8-13(12)23-16(15)18/h3-9,14,20H,2,18H2,1H3
Chemical Name	ethyl 2-amino-7-hydroxy-4-pyridin-3-yl-4H-chromene-3-carboxylate
Synonyms	HFI142; HFI 142; HFI-142
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]. Phenylalanine-544 plays a key role in substrate and inhibitor binding by providing a hydrophobicpacking point at the active site of insulin-regulated aminopeptidase. Mol Pharmacol. 2010 Oct;78(4):600-7.

Solubility Data

Solubility (In Vitro)

DMSO : ~125 mg/mL (~400.23 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (6.66 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 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 (6.66 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 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 (6.66 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 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	3.2018 mL	16.0092 mL	32.0184 mL
	5 mM	0.6404 mL	3.2018 mL	6.4037 mL
	10 mM	0.3202 mL	1.6009 mL	3.2018 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.