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Purity: ≥98%
Lafutidine (formerly FRG-8813; FRG8813; trade name: Protecadin; Stogar) is a 2nd-generation histamine H2 receptor antagonist used to treat gastric ulcers, duodenal ulcers, and wounds in the stomach associated with chronic gastritis. Lafutidine works by preventing the stomach acid from being secreted. It has been sold in India and Japan.
| Targets |
Histamine H2 receptor
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|---|---|---|
| ln Vitro |
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| ln Vivo |
Lafutidine (3-30 mg/kg; p.o.; twice daily; for 6 days) significantly mitigates changes in colon length and myeloperoxidase (MPO) activity, and reduces the severity of colitis induced by dextran sulfate Na (DSS) in a dose-dependent manner[3].
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| Animal Protocol |
Male Wistar rats (180-200 g)
3 mg/kg, 10 mg/kg, 30 mg/kg Oral administration, twice daily, for 6 days |
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| References |
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| Molecular Formula |
C22H29N3O4S
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|---|---|
| Molecular Weight |
431.55
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| Exact Mass |
431.19
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| Elemental Analysis |
C, 61.23; H, 6.77; N, 9.74; O, 14.83; S, 7.43
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| CAS # |
118288-08-7
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| Related CAS # |
(Z)-Lafutidine; 206449-93-6; Lafutidine-d10; 1795136-26-3
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| Appearance |
Solid powder
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| SMILES |
C1CCN(CC1)CC2=CC(=NC=C2)OC/C=C\CNC(=O)CS(=O)CC3=CC=CO3
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| InChi Key |
KMZQAVXSMUKBPD-DJWKRKHSSA-N
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| InChi Code |
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-
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| Chemical Name |
2-(furan-2-ylmethylsulfinyl)-N-[(Z)-4-[4-(piperidin-1-ylmethyl)pyridin-2-yl]oxybut-2-enyl]acetamide
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| Synonyms |
FRG-8813; Lafutidine; FRG8813; FRG 8813; trade name: Protecadin; Stogar
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (6.95 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 30.0 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: ≥ 3 mg/mL (6.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3 mg/mL (6.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3172 mL | 11.5861 mL | 23.1723 mL | |
| 5 mM | 0.4634 mL | 2.3172 mL | 4.6345 mL | |
| 10 mM | 0.2317 mL | 1.1586 mL | 2.3172 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02581696 | Completed | Drug: Lafutidine Drug: Irsogladine maleate |
Peptic Ulcer | Boryung Pharmaceutical Co., Ltd |
August 2015 | Phase 1 |
| NCT02658864 | Completed | Drug: lafutidine | Chronic Gastritis | Wuhan Union Hospital, China | April 2005 | Phase 1 |
| NCT01499368 | Completed | Drug: Lafutidine Drug: Famotidine Drug: Omeprazole |
Erosive Esophagitis | Boryung Pharmaceutical Co., Ltd |
November 2011 | Phase 3 |
| NCT02759224 | Completed | Drug: BRI-1501 Drug: Lafutidine Drug: Irsogladine maleate |
Gastric Ulcer | Boryung Pharmaceutical Co., Ltd |
April 15, 2016 | Phase 1 |
| NCT00229424 | Completed | Drug: Lafutidine Drug: Famotidine Other: Placebo |
Gastroesophageal Reflux | Taiho Pharmaceutical Co., Ltd. |
April 2005 | Phase 3 |
Products are for research use only; We do not sell to patients
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