FRG8701 |
Catalog No.GC32050 |
FRG-8701 is a new Histamine H2-receptor antagonist with an IC50 of ranging from 0.25 to 0.43 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 108498-50-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | In this study, male guinea pigs weighing 250-350 g are used. The hearts are excised from animals and right atria are dissected carefully. Atria are suspended in Krebs Henseleit (KH) solution, maintained at 32°C and aerated with 95% O2 and 5% CO2. The tissue is attached with an initial load of 1 g to an isometric transducer and allowed to stabilize for 60 min before histamine application. The histamine response is repeated 10 min after the tissue is incubated with various concentrations of FRG8701 or reference H2-antagonist[1]. |
Animal experiment: | Gastric mucosal lesions are produced using various kinds of necrotizing agents. One hour after necrotizing agent treatment, the animals are sacrificed. The stomach is removed and in flated by injecting 10 mL of 2% formalin. Subsequently, the stomach is incised along the curvature and examined for macroscopic hemorrhagic damages under a dissecting microscope (×10). In addition, FRG8701 is given intraperitoneally before HCI-ethanol treatment[1]. |
References: [1]. Shibata M,et al. Effects of FRG-8701 on gastric acid secretion, gastric mucosal lesions by necrotizing agents and experimental gastric or duodenal ulcer in rats. Jpn J Pharmacol. 1990 Nov;54(3):277-85. |
FRG-8701 is a new Histamine H2-receptor antagonist with an IC50 of ranging from 0.25 to 0.43 μM.
Positive chronotropic response to histamine at 10-5 M is dose dependently inhibited by FRG8701 (FRG-8701) famotidine or cimetidine; and the IC50 values of FRG8701, famotidine and cimetidine are 3.3, 3.0 and 108.6 (×10-7M), respectively.The inhibitory potency of FRG8701 is almost the same as that of famotidine and approximately 33 times greater than that of cimetidine[1].
In the pylorus-ligated (4 hr) rats, each drug, given intraduodenally, dose-dependently inhibits the total acid output. FRG8701 at 10 or 30 mg/kg, given orally or intraperitoneally, significantly prevent the formation of the gastric mucosal lesions induced by 0.4 N HCI+50% ethanol (HCI•ethanol). Other necrotizing agents-induced gastric lesions are also inhibited by treatment of FRG8701. The oral ED50 values against the lesions range from 1.1 to 9.4 mg/kg. FRG8701, given orally, dose-dependently prevents the development of gastric lesions induced by stress and indomethacin. Duodenal ulcer induced by mepirizole is also inhibited with FRG8701. The ED50 values of FRG8701 for each ulcer model range from 1.7 to 6.9 mg/kg[1].
[1]. Shibata M,et al. Effects of FRG-8701 on gastric acid secretion, gastric mucosal lesions by necrotizing agents and experimental gastric or duodenal ulcer in rats. Jpn J Pharmacol. 1990 Nov;54(3):277-85.
Cas No. | 108498-50-6 | SDF | |
Canonical SMILES | O=C(NCCCOC1=CC=CC(CN2CCCCC2)=C1)CS(CC3=CC=CO3)=O | ||
Formula | C22H30N2O4S | M.Wt | 418.55 |
Solubility | Soluble 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.3892 mL | 11.946 mL | 23.892 mL |
5 mM | 0.4778 mL | 2.3892 mL | 4.7784 mL |
10 mM | 0.2389 mL | 1.1946 mL | 2.3892 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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 ddH2O, 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.
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