Lafutidine (Synonyms: FRG 8813, (+)-Lafutidine) |
Catalog No.GC16085
One-Click Copy Product Info
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Histamine H2-receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 118288-08-7
Sample solution is provided at 25 µL, 10mM.
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Lafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.Target: histamine H(2)-receptorLafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.It is currently marketed in Japan (Stogar) China (Lemeiting) and India (Lafaxid). It not only suppresses gastric acid secretion, but also has cytoprotective properties by the virtue of its property to induce the collagen synthesis in the gastric mucosa. It has a novel mechanism of action in addition to blocking the H2 receptors, it decreases inflammation by modulating calcitonin gene-related peptide (CGRP) and vanilloid receptors. It is also found to stimulate mucin biosynthesis and promote the restitution of damaged mucosa.Lafutidine is absorbed in the small intestine, reaches gastric cells via the systemic circulation, and then directly and rapidly binds to gastric cell histamine H2 receptors, thereby inhibiting the stimulation of cAMP and a resultant decrease in acid production (antisecretory action). It causes a sustained increase in intracellular Ca2+ ion concentration in endothelial cells resulting in the release of Calcitonin Gene Related Peptide (CGRP), which causes acid suppression by decreasing the vagal tone. Lafutidine also increases plasma somatostatin levels which decreases secretion of gastrin from G cells. This decrease in gastrin causes inhibition of parietal cells, resulting in decrease in gastric acid secretion.
References:
[1]. Tanaka M, et al. Pharmacological and therapeutic properties of lafutidine (stogar and protecadin), a novel histamine H2 receptor antagonist with gastroprotective activity. Nihon Yakurigaku Zasshi. 2001 Jun;117(6):377-86.
| Cas No. | 118288-08-7 | SDF | |
| Synonyms | FRG 8813, (+)-Lafutidine | ||
| Chemical Name | 2-(furan-2-ylmethylsulfinyl)-N-[(Z)-4-[4-(piperidin-1-ylmethyl)pyridin-2-yl]oxybut-2-enyl]acetamide | ||
| Canonical SMILES | C1CCN(CC1)CC2=CC(=NC=C2)OCC=CCNC(=O)CS(=O)CC3=CC=CO3 | ||
| Formula | C22H29N3O4S | M.Wt | 431.55 |
| Solubility | ≥ 21.58mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3172 mL | 11.5861 mL | 23.1723 mL |
| 5 mM | 463.4 μL | 2.3172 mL | 4.6345 mL |
| 10 mM | 231.7 μL | 1.1586 mL | 2.3172 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)