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拉呋替丁 /Lafutidine {[allProObj[0].p_purity_real_show]}

货号：A101474 同义名： FRG-8813;(+)-Lafutidine

Lafutidine is an antagonist of histamine H(2)-receptor that inhibits gastric acid secretion.

Lafutidine 化学结构 CAS号：118288-08-7
Lafutidine 化学结构
CAS号：118288-08-7
Lafutidine 3D分子结构
CAS号：118288-08-7
Lafutidine 化学结构 CAS号：118288-08-7
Lafutidine 3D分子结构 CAS号：118288-08-7
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Lafutidine 纯度/质量文件 产品仅供科研

货号：A101474 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 H1 receptor ↓ H2 receptor ↓ H3 receptor ↓ H4 receptor ↓ Histamine receptor ↓ 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine ✔ 97%
Loratadine +

B(0)AT2, IC50: 4 μM

 		98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

 		98%
Doxylamine succinate ✔ 99%
Ebastine ✔ 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

 		98%
Meclizine dihydrochloride ✔ 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

 		99%
Diphenhydramine HCl ✔ 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

 		++

H2 receptor, pKi: 7.2

 		99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

 		99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

 		98%
Pemirolast potassium ✔ 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

 		98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

 		98%
Brompheniramine maleate ✔ 98%
Carbinoxamine maleate salt ✔ 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

 		98%
Ketotifen fumarate salt ✔ 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

 		PAFR 98%
Famotidine ✔ 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

 		98%
Lafutidine ✔ 99%
Cimetidine ✔ 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

 		AChE 98%
Ranitidine ✔ 99%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

 		98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

 		98%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 98%
Levodropropizine ✔ 97%
Cyproheptadine hydrochloride ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin hydrochloride ✔ 99+%
Buclizine 2HCl ✔ 97%
Latrepirdine 2HCl ✔ GluR 98%
Cetirizine 2HCl ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Lafutidine 生物活性

靶点

  • H2 receptor
描述 Lafutidine, a histamine H2 receptor antagonist with mucosal protective properties via sensory afferent neurons, is used for the treatment of upper gastrointestinal diseases. Daily administration of lafutidine reduced the severity of intestinal mucositis, diarrhea and body weight loss in a dose-dependent manner. Lafutidine attenuates 5-FU-induced intestinal mucositis, most likely by increasing mucus production via activation of sensory afferent neurons[3]. Lafutidine exhibited potent and long-lasting H2 antagonism and prolonged antisecretion. Lafutidine showed antiulcer activities against acute ulcer models, prevented gastric ulcer relapse of acetic ulcer, and accelerated the healing of indomethacin-induced antral ulcers in rats[4]. Intracisternal injection of RX 77368 (1.5 ng) or intraportal lafutidine (10 mg/kg) by itself did not affect hepatic blood flow, but co-injection of intracisternal RX 77368 (1.5 ng) and intraportal lafutidine (5 mg/kg) increased it with peak response at 30 min postinjection. The effect of lafutidine on hepatic blood flow in rats given RX 77368 was dose-related over the range 1 - 5 mg/kg[5]. Lafutidine, however, was superior to famotidine in terms of symptom relief of reflux esophagitis[6].

Lafutidine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02703896 Pulmonary Aspiration of Gastri... 展开 >>c Contents 收起 << Phase 4 Completed - -
NCT02555852 - Completed - Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 <<
NCT00229424 Gastroesophageal Reflux Phase 3 Completed - Japan ... 展开 >> Tohoku University Hospital 1-1, Seiryo-cho, Aoba-ku, Sendai, Miyagi, Japan, 980-8574 收起 <<

Lafutidine 参考文献

[1]Namikawa T, Munekage E, et al. Feasibility study of supportive care using lafutidine, a histamine H2 receptor antagonist, to prevent gastrointestinal toxicity during chemotherapy for gastric cancer. Anticancer Res. 2014 Dec;34(12):7297-301.

[2]Tanaka M, Banba M, et al. Pharmacological and therapeutic properties of lafutidine (stogar and protecadin), a novel histamine H2 receptor antagonist with gastroprotective activity. Nihon Yakurigaku Zasshi. 2001 Jun;117(6):377-86.

[3]Sano T, Utsumi D, Amagase K, Matsumoto K, Tominaga M, Higuchi K, Takeuchi T, Kato S. Lafutidine, a histamine H2 receptor antagonist with mucosal protective properties, attenuates 5-fluorouracil-induced intestinal mucositis in mice through activation of extrinsic primary afferent neurons. J Physiol Pharmacol. 2017 Feb;68(1):79-90

[4]Tanaka M, Banba M, Joko A, Moriyama Y. [Pharmacological and therapeutic properties of lafutidine (stogar and protecadin), a novel histamine H2 receptor antagonist with gastroprotective activity]. Nihon Yakurigaku Zasshi. 2001 Jun;117(6):377-86. Japanese

[5]Yoneda M, Kurosawa M, Watanobe H, Terano A. Lafutidine increases hepatic blood flow via potentiating the action of central thyrotropin-releasing hormone in rats. J Gastroenterol Hepatol. 2003 Feb;18(2):177-84

[6]Kim EH, Lee YC, Chang YW, Park JJ, Chun HJ, Jung HY, Kim HS, Jeong HY, Seol SY, Han SW, Choi MG, Park SH, Lee OJ, Jung JT, Lee DH, Jung HC, Lee ST, Kim JG, Youn SJ, Kim HY, Lee SW. Efficacy of Lafutidine Versus Famotidine in Patients with Reflux Esophagitis: A Multi-Center, Randomized, Double-Blind, Non-inferiority Phase III Trial. Dig Dis Sci. 2015 Jun;60(6):1724-32

Lafutidine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.59mL

2.32mL

1.16mL

23.17mL

4.63mL

2.32mL

Lafutidine 技术信息

CAS号118288-08-7
分子式C22H29N3O4S
分子量 431.548
别名 FRG-8813;(+)-Lafutidine
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 50 mg/mL(115.86 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Lafutidine | 118288-08-7 | FRG-8813 | FRG8813 | FRG 8813 | H2RA Antagonist | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Histamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Lafutidine 纯度/质量文件 | Lafutidine 亚型比较 | Lafutidine 生物活性 | Lafutidine 临床数据 | Lafutidine 参考文献 | Lafutidine 实验方案 | Lafutidine 技术信息

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