Zastaprazan (JP-1366) is a proton pump inhibitor (WO2018008929). Zastaprazan is indicated for the study of gastrointestinal inflammation or stomach acid-related disorders.

Physicochemical Properties

Molecular Formula	C22H26N4O
Molecular Weight	362.468044757843
Exact Mass	362.21
Elemental Analysis	C, 72.90; H, 7.23; N, 15.46; O, 4.41
CAS #	2133852-18-1
Related CAS #	2936619-43-9 (citrate)
PubChem CID	138622158
Appearance	White to off-white solid powder
LogP	4.4
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	4
Heavy Atom Count	27
Complexity	526
Defined Atom Stereocenter Count	0
SMILES	O=C(C1C=C(C2=NC(C)=C(C)N2C=1)NCC1C(C)=CC=CC=1C)N1CCC1
InChi Key	FEQFUBYYZYQTOJ-UHFFFAOYSA-N
InChi Code	InChI=1S/C22H26N4O/c1-14-7-5-8-15(2)19(14)12-23-20-11-18(22(27)25-9-6-10-25)13-26-17(4)16(3)24-21(20)26/h5,7-8,11,13,23H,6,9-10,12H2,1-4H3
Chemical Name	azetidin-1-yl-[8-[(2,6-dimethylphenyl)methylamino]-2,3-dimethylimidazo[1,2-a]pyridin-6-yl]methanone
Synonyms	Zastaprazan; 2133852-18-1; Zastaprazan [INN]; W9S9KZX5MD; Zastaprazan (INN);
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	Proton pump[1]
ln Vitro	Zastaprazan is a small molecule therapeutic agent. The presence of the International Nonproprietary Name stem "-prazan" in its nomenclature classifies it as a proton pump inhibitor that operates independently of acid-activated conversion. Currently, Zastaprazan is being evaluated in clinical study NCT05814809, a trial designed to assess its safety profile and pharmacokinetic characteristics in healthy adult participants. The compound possesses a monoisotopic molecular mass of 362.21 Daltons.
References	[1]. WO2018008929.

Solubility Data

Solubility (In Vitro)

DMSO: 33.33 mg/mL (91.95 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.90 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 (6.90 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	2.7588 mL	13.7942 mL	27.5885 mL
	5 mM	0.5518 mL	2.7588 mL	5.5177 mL
	10 mM	0.2759 mL	1.3794 mL	2.7588 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.