Lansoprazole Inhibitor CAS No. 103577-45-3

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KI0829	Lansoprazole	50 mg	$154

Chemical Characteristic

Product Name	Lansoprazole
Synonyms	Prevacid, AG-1749
CAS No.	103577-45-3
Molecular Weight	369.36
Formula	C₁₆H₁₄F₃N₃O₂S
Chemical Structure

Biological activities

Lansoprazole is a proton-pump inhibitor. Lansoprazole inhibits the stomach's production of gastric acids. Lansoprazole inhibits digoxin transport with an IC50 of 62.8 µM. Lansoprazole competitively inhibits CYP2C19 activity with a K_{i ranging from 0.4 to 1.5 µM.^[2] Lansoprazole inhibits dibutyryl-cAMP-stimulated acid formation and (H⁺+ K⁺)-ATPase with IC50 of 59 nM and 2.1 µM, respectively.^[3] Lansoprazole at the dose of 300 µM inhibits Ca²⁺-induced contractions in high K⁺-Ca²⁺ free medium.^[4] Lansoprazole competitively inhibits CYP2C9-catalyzed conversion of tolbutamide to 4-hydroxytolbutamide with a K_{i of 52.1 µM. Lansoprazole noncompetitively inhibits CYP3A-catalyzed conversion of dextromethorphan to 3-methoxymorphinan with a K_{i of 170.4 µM.^[5] Lansoprazole administration increases VEGF expression at the ulcer margin in a dose-dependent manner.^[6] Lansoprazole significantly decreases proinflammatory cytokines in mRNA and protein expression.^[7] Lansoprazole markedly inhibits acid secretion in pylorus-ligated rats.^[8] Lansoprazole decreases testosterone responsiveness in rats.^[9]}}}

Protocols

In vitro: Lansoprazole is dissolved in DMSO.^[7]

References

[1] Pauli-Magnus C, et al. Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein. Naunyn Schmiedebergs Arch Pharmacol. 2001, 364(6): 551-557. 閵嗏偓閵嗏偓 [2] Li XQ, et al. Comparison of inhibitory effects of the proton pump-inhibiting drugs omeprazole, esomeprazole, lansoprazole, pantoprazole, and rabeprazole on human cytochrome P450 activities. Drug Metab Dispos. 2004, 32(8): 821-827. 閵嗏偓閵嗏偓 [3] Nagaya H, et al. Effects of the enantiomers of lansoprazole (AG-1749) on (H+ + K⁺)-ATPase activity in canine gastric microsomes and acid formation in isolated canine parietal cells. Biochem Pharmacol. 1991, 42(10): 1875-1878. 閵嗏偓閵嗏偓 [4] Naseri E, et al. Proton pump inhibitors omeprazole and lansoprazole induce relaxation of isolated human arteries. Eur J Pharmacol. 2006, 531(1-3): 226-231. 閵嗏偓閵嗏偓 [5] Ko JW, et al. Evaluation of omeprazole and lansoprazole as inhibitors of cytochrome P450 isoforms. Drug Metab Dispos. 1997, 25(7): 853-862. 閵嗏偓閵嗏偓 [6] Kobayashi S, et al. Effects of lansoprazole on the expression of VEGF and cellular proliferation in a rat model of acetic acid-induced gastric ulcer. J Gastroenterol. 2010, 45(8): 846-858. 閵嗏偓閵嗏偓 [7] Hinoki A, et al. Suppression of proinflammatory cytokine production in macrophages by lansoprazole. Pediatr Surg Int. 2006, 22(11): 915-923. [8] Blandizzi C, et al. Lansoprazole prevents experimental gastric injury induced by non-steroidal anti-inflammatory drugs through a reduction of mucosal oxidative damage. World J Gastroenterol. 2005, 11(26): 4052-4060. 閵嗏偓閵嗏偓 [9] Fort FL, et al. Mechanism for species-specific induction of Leydig cell tumors in rats by lansoprazole. Fundam Appl Toxicol. 1995, 26(2): 191-202. 閵嗏偓閵嗏偓

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