[CAS NO. 161973-10-0] Esomeprazole magnesium

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PRODUCTS SPECIFICATIONS [161973-10-0]

Catalog

HY-B1446

Brand

MCE

CAS

161973-10-0

DESCRIPTION [161973-10-0]

Overview

MDL	MFCD06798050
Molecular Weight	713.12
Molecular Formula	C34H36MgN6O6S2
SMILES	CC1=C(N=CC(C)=C1OC)CS2=O[Mg+2]3([N](C4=CC=C(OC)C=C4[N-]5)=C5S(CC(N=CC(C)=C6OC)=C6C)=O3)[N]7=C2[N-]C8=CC(OC)=CC=C78

For research use only. We do not sell to patients.

Summary

Esomeprazole magnesium ((S)-Omeprazole magnesium) is a potent and orally active H ⁺ , K ⁺ -ATPase inhibitor. Esomeprazole magnesium has the potential for upper intestinal disorders and gastroesophageal reflux disease research ^[1] ^[2] . Esomeprazole magnesium acts as an exosome inhibitor by blocking the exosome release via the inhibition of V-H ⁺ -ATPases ^[4] .

IC50 & Target

H ⁺ , K ⁺ -ATPase ^[1]

In Vitro

Esomeprazole magnesium is an inhibitor of H ⁺ , K ⁺ -ATPase ^[1] .Esomeprazole magnesium is develped from Esomeprazole strontium tetrahydrate (EST). EST contains esomeprazole, the S-enantiomer of omeprazole a salt-exchanged version of Esomeprazole magnesium trihydrate ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Esomeprazole magnesium (0.5-50 mg/kg; oral gavage; daily; for 10 days; A/J mice) treatment increases gastric total antioxidant capacity and Cu/Zn-superoxide dismutase activity ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	A/J mice ^[1]
Dosage:	0.5 mg/kg, 5 mg/kg, 50 mg/kg
Administration:	Oral gavage; daily; for 10 days
Result:	Gastric total antioxidant capacity and Cu/Zn-superoxide dismutase activity are increased.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02680132	Torrent Pharmaceuticals Limited	Healthy	May 2011	Phase 1
NCT00206180	AstraZeneca	Erosive Esophagitis\|Reflux Esophagitis\|Gastroesophageal Reflux Disease	June 2004	Phase 4
NCT01135472	City of Hope Medical Center	Healthy	March 2010	Phase 1
NCT00637559	AstraZeneca	Barrett´s Esophagus	March 2002	Phase 4
NCT00079833	AstraZeneca	Zollinger-Ellison Syndrome	November 2003	Phase 3
NCT02659683	Torrent Pharmaceuticals Limited	Healthy Subjects	May 2011	Phase 1
NCT01142128	University of Florida\|AstraZeneca	Chronic Pancreatitis	February 2009	Phase 1
NCT00443963	Medstar Health Research Institute\|AstraZeneca	Dyspepsia	December 2006	Phase 4
NCT00637845	AstraZeneca	Heartburn\|Gastroesophageal Reflux Disease	June 2002	Phase 4
NCT02680119	Torrent Pharmaceuticals Limited	Healthy	May 2011	Phase 1
NCT04696783	Fifth Affiliated Hospital, Sun Yat-Sen University	Gastroesophageal Reflux Disease	July 2021	Phase 3
NCT00687245	AstraZeneca	Endoscopically-Proven GERD\|Reflux	August 2006	Phase 1
NCT00474903	National Cancer Institute (NCI)	Barrett Esophagus\|Esophageal Cancer	April 2007	Phase 2
NCT00206024	AstraZeneca	Heartburn	November 2004	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 125 mg/mL ( 175.29 mM )

H ₂ O : 3 mg/mL ( 4.21 mM ; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.4023 mL	7.0114 mL	14.0229 mL
5 mM	0.2805 mL	1.4023 mL	2.8046 mL
10 mM	0.1402 mL	0.7011 mL	1.4023 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (2.92 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (2.92 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (2.92 mM); Clear solution
4.

Add each solvent one by one: PBS

Solubility: 1.43 mg/mL (2.01 mM); Clear solution; Need ultrasonic

* All of the co-solvents are available by MCE.

References

Synonyms

Magnesium, bis[6-methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl-κO]-1H-benzimidazolato-κN³]-, (T-4)-

Magnesium, bis[5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazolato]-, [T-4-(S),(S)]-

(T-4)-Bis[6-methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl-κO]-1H-benzimidazolato-κN³]magnesium

Esomeprazole magnesium

H 199/18

Nexium

(-)-Omeprazole magnesium

(S)-Omeprazole magnesium

Perprazole

Raciper