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

Roxatidine Acetate Hydrochloride  (Synonyms: 盐酸罗沙替丁醋酸酯; HOE 760)

目录号: HY-B0305A 纯度: 99.26%
COA 产品使用指南

Roxatidine Acetate Hydrochloride 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 Hydrochloride 对胃酸分泌有抗分泌作用。Roxatidine Acetate Hydrochloride 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 Hydrochloride 具有抗肿瘤活性。

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Roxatidine Acetate Hydrochloride Chemical Structure

Roxatidine Acetate Hydrochloride Chemical Structure

CAS No. : 93793-83-0

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10 mM * 1 mL in DMSO ¥660
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500 mg ¥600
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1 g ¥980
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5 g ¥2800
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Other Forms of Roxatidine Acetate Hydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target[1]

H2 Receptor

 

体外研究
(In Vitro)

Roxatidine Acetate Hydrochloride (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 Hydrochloride (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 Hydrochloride (0-300 mg/kg; p.o.; 26 days) suppressed growth of Colon 38 tumor implants in mice[3].
Roxatidine Acetate Hydrochloride (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 Acetate Hydrochloride 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)[1]
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

384.90

Formula

C19H29ClN2O4

CAS 号
性状

固体

颜色

White to off-white

中文名称

盐酸罗沙替丁醋酸酯;盐酸醋酸罗沙替丁

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 50 mg/mL (129.90 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : ≥ 50 mg/mL (129.90 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5981 mL 12.9904 mL 25.9808 mL
5 mM 0.5196 mL 2.5981 mL 5.1962 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 140 mg/mL (363.73 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献

Roxatidine Acetate Hydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.5981 mL 12.9904 mL 25.9808 mL 64.9519 mL
5 mM 0.5196 mL 2.5981 mL 5.1962 mL 12.9904 mL
10 mM 0.2598 mL 1.2990 mL 2.5981 mL 6.4952 mL
15 mM 0.1732 mL 0.8660 mL 1.7321 mL 4.3301 mL
20 mM 0.1299 mL 0.6495 mL 1.2990 mL 3.2476 mL
25 mM 0.1039 mL 0.5196 mL 1.0392 mL 2.5981 mL
30 mM 0.0866 mL 0.4330 mL 0.8660 mL 2.1651 mL
40 mM 0.0650 mL 0.3248 mL 0.6495 mL 1.6238 mL
50 mM 0.0520 mL 0.2598 mL 0.5196 mL 1.2990 mL
60 mM 0.0433 mL 0.2165 mL 0.4330 mL 1.0825 mL
80 mM 0.0325 mL 0.1624 mL 0.3248 mL 0.8119 mL
100 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6495 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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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产品名称:
Roxatidine Acetate Hydrochloride
目录号:
HY-B0305A
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