1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Roxatidine acetate

Roxatidine acetate  (Synonyms: 醋酸罗沙替丁)

目录号: HY-B0305
产品使用指南

Roxatidine acetate 是一种有效的、选择性的、竞争性的、具有口服活性的组胺 H2 受体(histamine H2-receptor)拮抗剂。Roxatidine acetate 对胃酸分泌有抗分泌作用。Roxatidine acetate 还能抑制炎症反应,可用于胃溃疡和十二指肠溃疡的研究。Roxatidine acetate 具有抗肿瘤活性。

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Roxatidine acetate Chemical Structure

Roxatidine acetate Chemical Structure

CAS No. : 78628-28-1

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Roxatidine acetate 的其他形式现货产品:

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  • 生物活性

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  • 参考文献

生物活性

Roxatidine acetate is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity[1][2][3].

IC50 & Target

H2 Receptor

 

体外研究
(In Vitro)

Roxatidine acetate (0-120 μM, 1 h) suppresses inflammatory responses via inhibition of NF-κB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages[2].
Roxatidine acetate (6.25  μM, 12.5 μM, and 25 μM; pre-treatment for 30 min) suppresses the PMACI-induced activation of p38 MAPK, but does not affect the phosphorylation of ERK or JNK. The total ERK 1/2, JNK, and p38 MAPK levels are unaffected by roxatidine in human mast-cells-1 (HMC-1) cells[4].

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

Western Blot Analysis[2]

Cell Line: RAW 264.7
Concentration: 40, 80, and 120 μM
Incubation Time: 1 h
Result: Suppressed LPS-induced PGE2, NO, and histamine production and COX-2, iNOS, and HDC expressions. Inhibited expressions of TNF-α, IL-1β, IL-6, and VEGF-1. Concentration-dependently attenuated the nuclear translocations of p65 and p50. Inhibited LPS-induced phosphorylation of p38 MAP kinase. Significantly down-regulated the LPS-induced productions of NO and PGE2 (prostaglandin E2).
体内研究
(In Vivo)

Roxatidine acetate (0-300 mg/kg; p.o.; 26 days) suppressed growth of Colon 38 tumor implants in mice[3].
Roxatidine acetate (oral gavage; 20 mg/kg; single dose) inhibits Compound 48/80-increased TNF-α, IL-6, and IL-1β production and mRNA expression. Additionally, Roxatidine decreases the compound 48/80-induced degradation of procaspase-1 and appearance of the corresponding cleaved bands in mice[4].

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

Animal Model: Male C57BL/6 Colon 38-bearing mice (8-week-old, 20 – 22 g)[3]
Dosage: 30, 100, and 300 mg/kg per day, 1 ml/100 g body weight
Administration: Oral administration, 29 days beginning 3 days before Colon 38 implantation or 26 days beginning concomitantly with Colon 38 implantation
Result: Suppressed growth of Colon 38 tumor implants in a dose-related manner after day 26. Suppressed VEGF levels in tumor tissue and significantly decreased serum VEGF levels.
Animal Model: ICR male mice (6 weeks old)[4]
Dosage: 20 mg/kg
Administration: Oral gavage; 20 mg/kg; single dose
Result: Suppressed compound 48/80-induced allergic inflammation in anaphylactic animal model.
分子量

348.44

Formula

C19H28N2O4

CAS 号
中文名称

醋酸罗沙替丁

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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The molarity calculator equation

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Roxatidine acetate
目录号:
HY-B0305
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