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Cat. No.: HY-U00238

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FRG8701

FRG-8701 is a new Histamine H₂-receptor antagonist with an IC₅₀ of ranging from 0.25 to 0.43 μM.

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

CAS No.: 108498-50-6
Formula: C₂₂H₃₀N₂O₄S
Molecular Weight:418.55

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

FRG8701 Chemical Structure

CAS No.: 108498-50-6

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

FRG-8701 is a new Histamine H₂-receptor antagonist with an IC₅₀ of ranging from 0.25 to 0.43 μM.

IC₅₀ & Target

IC50: 0.25 to 0.43 μM (Histamine H₂-receptor)^[1]

All Histamine Receptor Isoforms :

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

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].

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

Chemical Information

CAS No. 108498-50-6
Molecular Weight 418.55
Formula C₂₂H₃₀N₂O₄S
SMILES

O=C(NCCCOC1=CC=CC(CN2CCCCC2)=C1)CS(CC3=CC=CO3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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