(+)-Lafutidine

(+)-Lafutidine is an antagonist of histamine H2-receptor that inhibits gastric acid secretion

Product information

CAS Number: 118288-08-7

Molecular Weight: 431.55

Formula: C22H29N3O4S

Synonym:

FRG-8813

Chemical Name: 2-(furan-2-ylmethylsulfinyl)-N-[(Z)-4-[4-(piperidin-1-ylmethyl)pyridin-2-yl]oxybut-2-enyl]acetamide

Smiles: O=C(CS(=O)CC1=CC=CO1)NC/C=C\COC1=CC(CN2CCCCC2)=CC=N1

InChiKey: KMZQAVXSMUKBPD-DJWKRKHSSA-N

InChi: InChI=1S/C22H29N3O4S/c26-21(18-30(27)17-20-7-6-14-28-20)23-9-2-5-13-29-22-15-19(8-10-24-22)16-25-11-3-1-4-12-25/h2,5-8,10,14-15H,1,3-4,9,11-13,16-18H2,(H,23,26)/b5-2-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 86 mg/mL(199.28 mM). Water: Insoluble.

Shipping Condition: Shipped under ambien...

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Lafutidine exhibits gastric mucosal protective action mediated by capsaicin-sensitive afferent neurons, in addition to a potent antisecretory effect[2]. Lafutidine (0.1-10 µM) significantly augments the periarterial nerve stimulation (PNS, 1 Hz) induced-vasodilation in a concentration-dependent manner in rat perfused mesenteric vascular beds[2].

In Vivo:

Lafutidine (3-30 mg/kg; p.o.; twice daily; for 6 days) dose-dependently reduces the severity of dextran sulfate Na (DSS)-induced colitis and significantly mitigates changes in the colon length and myeloperoxidase (MPO) activity[3].

References:

1. Motoko Nakano, et al. Possible involvement of host defense mechanism in the suppression of rat acute reflux esophagitis by the particular histamine H2 receptor antagonist lafutidine. Pharmacology. 2012;90(3-4):205-11.
2. Tetsuhiro Sugiyama, et al. Lafutidine facilitates calcitonin gene-related peptide (CGRP) nerve-mediated vasodilation via vanilloid-1 receptors in rat mesenteric resistance arteries. J Pharmacol Sci. 2008 Mar;106(3):505-11.
3. Mitsuaki Okayama, et al. Protective effect of lafutidine, a novel histamine H2-receptor antagonist, on dextran sulfate sodium-induced colonic inflammation through capsaicin-sensitive afferent neurons in rats. Dig Dis Sci. 2004 Oct;49(10):1696-704.

Products are for research use only. Not for human use.