Description
FRG-8701 is a new Histamine H2-receptor antagonist with an IC50 of ranging from 0.25 to 0.43 μM.
Product information
CAS Number: 108498-50-6
Molecular Weight: 418.55
Formula: C22H30N2O4S
Chemical Name: 2-[(furan-2-yl)methanesulfinyl]-N-(3-{3-[(piperidin-1-yl)methyl]phenoxy}propyl)acetamide
Smiles: O=C(CS(=O)CC1=CC=CO1)NCCCOC1C=C(CN2CCCCC2)C=CC=1
InChiKey: IWLUMUDDKHJJPB-UHFFFAOYSA-N
InChi: InChI=1S/C22H30N2O4S/c25-22(18-29(26)17-21-9-5-13-28-21)23-10-6-14-27-20-8-4-7-19(15-20)16-24-11-2-1-3-12-24/h4-5,7-9,13,15H,1-3,6,10-12,14,16-18H2,(H,23,25)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
Products are for research use only. Not for human use.
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