Lafutidine (Synonyms: FRG-8813)

Cat. No.: HY-B0160 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

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Lafutidine (FRG-8813) is a histamine H2-receptor antagonist (H₂RA), with proven gastric mucosal protective effects. Lafutidine can be used for the research of gastroesophageal reflux disease.

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

Lafutidine Chemical Structure

CAS No. : 118288-08-7

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25 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Other Forms of Lafutidine:

(Z)-Lafutidine Get quote
Lafutidine-d₁₀ Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Lafutidine (FRG-8813) is a histamine H2-receptor antagonist (H₂RA), with proven gastric mucosal protective effects. Lafutidine can be used for the research of gastroesophageal reflux disease^[1].

IC₅₀ & Target

Histamine H₂-receptor^[1]

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].

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

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].

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

Animal Model:	Male Wistar rats (180-200 g)^[3]
Dosage:	3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:	Oral administration, twice daily, for 6 days
Result:	Reduced the severity of DSS-induced ulcerative colitis in a dose-dependent manner.

Clinical Trial

Molecular Weight

431.55

Formula

C₂₂H₂₉N₃O₄S

CAS No.

118288-08-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC/C=C\COC1=NC=CC(CN2CCCCC2)=C1)CS(CC3=CC=CO3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (115.86 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (6.95 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (6.95 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (6.95 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (275 KB) SDS (0 KB)

COA (250 KB) LCMS (257 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3172 mL	11.5861 mL	23.1723 mL	57.9307 mL
	5 mM	0.4634 mL	2.3172 mL	4.6345 mL	11.5861 mL
	10 mM	0.2317 mL	1.1586 mL	2.3172 mL	5.7931 mL
	15 mM	0.1545 mL	0.7724 mL	1.5448 mL	3.8620 mL
	20 mM	0.1159 mL	0.5793 mL	1.1586 mL	2.8965 mL
	25 mM	0.0927 mL	0.4634 mL	0.9269 mL	2.3172 mL
	30 mM	0.0772 mL	0.3862 mL	0.7724 mL	1.9310 mL
	40 mM	0.0579 mL	0.2897 mL	0.5793 mL	1.4483 mL
	50 mM	0.0463 mL	0.2317 mL	0.4634 mL	1.1586 mL
	60 mM	0.0386 mL	0.1931 mL	0.3862 mL	0.9655 mL
	80 mM	0.0290 mL	0.1448 mL	0.2897 mL	0.7241 mL
	100 mM	0.0232 mL	0.1159 mL	0.2317 mL	0.5793 mL

Lafutidine Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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