1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Anti-infection
  2. Histamine Receptor SARS-CoV Bacterial
  3. Ranitidine bismuth citrate

Ranitidine bismuth citrate  (Synonyms: 枸椽酸铋雷尼替丁)

目录号: HY-B0693A
产品使用指南 技术支持

Ranitidine 是一种强效、选择性、具有口服活性的组胺 H2 受体 (histamine H2-receptor) 拮抗剂,可抑制胃液分泌。Ranitidine 可拮抗 Histamine (HY-B1204) 诱导的豚鼠离体大鼠心房扩张和组胺诱导的大鼠离体子宫角松弛,pA2 值分别为 7.2 和 6.95。Ranitidine 对 SARS-CoV-2 感染细胞具有选择性。Ranitidine 还具有抗幽门螺杆菌感染的作用。Ranitidine 可抑制小鼠乳腺肿瘤的发展和扩散。

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Ranitidine bismuth citrate Chemical Structure

Ranitidine bismuth citrate Chemical Structure

CAS No. : 128345-62-0

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ranitidine bismuth citrate is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine bismuth citrate antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine bismuth citrate has selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate also has anti-Helicobacter pylori infection. Ranitidine bismuth citrate inhibits breast tumor development and spread in mice[1][2][3][4].

IC50 & Target

H2 Receptor

 

体外研究
(In Vitro)

Ranitidine bismuth citrate (0.1-1 μM,5 分钟) 是 SARS-CoV-2 解旋酶的 ATPase (IC50 = 0.69 μM,Ki = 0.97 μM) 和 DNA 解旋 (IC50 = 0.74 μM,Ki = 0.39 μM) 的强效不可逆抑制剂[2]
Ranitidine bismuth citrate (24 小时) 对 SARS-CoV-2 表现出强效活性,在 Vero E6 细胞中的 EC50 值为 2.3 μM[2]

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

Cell Cytotoxicity Assay[2]

Cell Line: Monkey kidney Vero E6 cells, human colorectal Caco-2 cells
Concentration: 400-3,740 μM
Incubation Time: 48 hours
Result: Showed low cytotoxicity with the 50% cytotoxicity concentrations (CC50) ranging from 2.2 mM and 2.5 mM.
体内研究
(In Vivo)

Ranitidine (0.03-3 mg/kg;静脉注射;一次) bismuth citrate 可抑制麻醉大鼠灌注胃制剂中 Histamine (HY-B1204) 和 Pentagastrin (HY-A0261) 诱导的胃酸分泌[1]
Ranitidine bismuth citrate (150 mg/kg;腹腔注射;每日一次;4 天) 可抑制 SARS-CoV-2 复制,并缓解金黄叙利亚仓鼠模型中的病毒相关肺炎[2]
在大鼠实验中,Ranitidine bismuth citrate (3-30 mg/kg,口服) 可预防乙醇引起的胃底损伤 (胃底损伤) 和吲哚美辛引起的胃窦损伤 (胃窦损伤)[3]
在自然寄生有鼬形水蚤 (H. mustelae) 的雪貂中,Ranitidine bismuth citrate (口服;12-24 mg/kg;每日两次;持续4周) 可导致剂量相关的鼬形水蚤 (H. mustelae) 清除率[3]
Ranitidine (8 mg/kg;口服;每隔一天给药;给药 8 天) bismuth citrate 在 BALB/c 小鼠的脾脏和骨髓中,使 CD11b+Ly6Chi细胞数量减少[4]
Ranitidine (8 mg/kg;口服;每隔一天给药;给药 8 天) bismuth citrate 在荷 4T1 乳腺癌的 BALB/c 小鼠中,抑制了肺转移[4]
Ranitidine (8 mg/kg;口服;每隔一天给药;给药 14 天) bismuth citrate 在 C57BL/6 小鼠的 E0771 乳腺癌模型中,抑制了原发性肿瘤生长[4]
Ranitidine (剂量使小鼠每天摄入 6-8 mg/kg;加入饮用水;每 3 天更换一次;从断奶开始 (约 4 周) 至实验结束 (23-26 周)) bismuth citrate 在 LKB1-/-NIC 小鼠中,增加了乳腺肿瘤发生的潜伏期并减少了肿瘤数量[4]

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

Animal Model: Female Wistar rats (100 to 120 g) were anaesthetized with sodium pentobarbitone (50 mg/kg i.p.), and intravenous with Histamine (100 μg/kg/min) or Pentagastrin (1 μg/kg/min)[1].
Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 0.6 mg/kg, 1 mg/kg, 3 mg/kg
Administration: i.v.; once
Result: Inhibited Histamine- and Pentagastrin-induced gastric acid secretion in the perfused stomach preparation of the anaesthetized rat.
Animal Model: Male and female Syrian hamsters (6-10 weeks)[2]
Dosage: 150 mg/kg
Administration: Intraperitoneally given; once daily; 4 days
Result: Suppressed SARS-CoV-2 replication, and relieved virus-associated pneumonia in a golden Syrian hamster model.
Animal Model: BALB/c female mice (5-6-8 week old), orthotopic breast cancer model by injecting 100,000 4T1 cells subcutaneously into the mammary fat pad near the fourth nipple[4].
Dosage: 8 mg/kg
Administration: Oral administration, every other day, 8 days
Result: Decreased the proportion of CD11b+Ly6Chi monocytic cells in the spleen and inhibited lung metastasis.
Animal Model: C57BL/6 female mice (6-8 week old), orthotopic breast cancer model by injecting 200,000 E0771 cells in 100 μL of Matrigel subcutaneously into the mammary fat pad near the fourth nipple[4].
Dosage: 8 mg/kg
Administration: Oral administration, every other day, 8 days
Result: Decreased primary tumor growth starting from approximately day 13 post-tumor cell injection.
Animal Model: LKB1-/-/NIC female mice (weaned at about 4 weeks old), spontaneous tumor development model starting from weaning[4].
Dosage: 6-8 mg/kg
Administration: Oral administration, every 3 days, from weaning until the end of the experiment
Result: Increased the latency of tumorigenesis by an additional 24 days and reduced the average number of tumors per mouse.
分子量

712.48

Formula

C19H27BiN4O10S

CAS 号
中文名称

枸椽酸铋雷尼替丁

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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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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Ranitidine bismuth citrate
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