FRG8701
FRG-8701 is a new Histamine H2-receptor antagonist with an IC50 of ranging from 0.25 to 0.43 μM.
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- CAS 番号: 108498-50-6
- 分子式: C22H30N2O4S
- 分子量:418.55
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
IC50: 0.25 to 0.43 μM (Histamine H2-receptor)[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 108498-50-6
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分子量 418.55
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分子式 C22H30N2O4S
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SMILES
O=C(NCCCOC1=CC=CC(CN2CCCCC2)=C1)CS(CC3=CC=CO3)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
FRG8701 関連分類
HY-U00238 関連分類
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