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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.

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CAS No.: 108498-50-6
화학식: C₂₂H₃₀N₂O₄S
분자량:418.55

보관:

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

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Protocol
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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.

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
분자량 418.55
화학식 C₂₂H₃₀N₂O₄S
SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

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

Protocol

Cell Assay^[1]

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.

Animal Administration^[1]

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.

순도&문서

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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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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Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Protocol
순도&문서
References

상품명:
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FRG8701

All Histamine Receptor Isoforms

Biological Activity

Chemical Information

Protocol

순도&문서

References

Calculators

Help & FAQs

FRG8701 Related Classifications

HY-U00238 Related Classifications

Bioz