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Famotidine/法莫替丁 {[allProObj[0].p_purity_real_show]}

货号:A701177 同义名: MK-208; YM-11170

Famotidine是一种组胺 H2 受体拮抗剂,可抑制胃酸分泌,IC50 为 0.6 mM,用于胃灼热和其他消化系统疾病的研究。

Famotidine/法莫替丁 化学结构 CAS号:76824-35-6
Famotidine/法莫替丁 化学结构
CAS号:76824-35-6
Famotidine/法莫替丁 3D分子结构
CAS号:76824-35-6
Famotidine/法莫替丁 化学结构 CAS号:76824-35-6
Famotidine/法莫替丁 3D分子结构 CAS号:76824-35-6
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Famotidine/法莫替丁 纯度/质量文件 产品仅供科研

货号:A701177 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 2HCl 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 96%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

99%
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

99%
Azelastine HCl 98%
Epinastine HCl 99%
Levodropropizine 97%
Cyproheptadine HCl 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin HCl 99+%
Buclizine 2HCl 95%
Latrepirdine 2HCl GluR 99%
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。

Famotidine/法莫替丁 生物活性

靶点
  • H2 receptor

描述 Famotidine is a histamine-2 receptor antagonists. Steers received IV famotidine (0.4 mg/kg) as a single and 3-dose regimen (every 8 hours) versus saline control. Abomasal outflow fluid pH was higher in steers treated with famotidine for up to 4 hours after a single dose but the effect decreased with subsequent doses. Famotidine may be useful for treatment or prevention of abomasal ulceration in adult cattle, but the duration of effect may decrease with time[2]. Continued administration of famotidine results in a diminished effect on intragastric pH in dogs[3]. A famotidine CRI (continuous rate infusion), but not standard doses of famotidine, achieves the clinical goals established in people to promote healing of gastric tissue injury and offers an alternative to intravenous treatment with proton pump inhibitors in dogs[4]. Oral famotidine administration results in a diminished effect on intragastric pH in healthy cats when given twice daily every day[5].

Famotidine/法莫替丁 细胞实验

Cell Line
Concentration Treated Time Description References
A549 cells 50 µM 12 hours Pretreatment of these cells with famotidine reduced TLR3 mRNA levels, but did not affect TLR7 expression. J Biol Chem. 2021 Aug;297(2):100925.
Caco2 cells 50 µM 12 hours Famotidine treatment inhibits histamine-induced expression of Toll-like receptor 3 (TLR3) in SARS-CoV-2 infected cells and can reduce TLR3-dependent signaling processes that culminate in activation of IRF3 and the NF-κB pathway, subsequently controlling antiviral and inflammatory responses. J Biol Chem. 2021 Aug;297(2):100925.
Mouse primary peritoneal macrophages 0 to 30 µM 16 hours To evaluate the inhibitory effect of famotidine on LPS-induced TNF and IL-6 release, results showed that famotidine did not significantly inhibit LPS-induced TNF and IL-6 release in mouse primary peritoneal macrophages. Mol Med. 2022 May 16;28(1):57.
RAW 264.7 cells 0 to 30 µM 16 hours To evaluate the inhibitory effect of famotidine on LPS-induced TNF and IL-6 release, results showed that famotidine did not significantly inhibit LPS-induced TNF and IL-6 release in RAW 264.7 cells. Mol Med. 2022 May 16;28(1):57.
Human lung A549 cells up to 200 µM 72 hours To assess the inhibitory effect of famotidine on SARS-CoV-2 replication in human lung cells, results showed no significant antiviral activity. Sci Rep. 2021 Mar 8;11(1):5433.
Vero E6 cells up to 200 µM 72 hours To evaluate the inhibitory effect of famotidine on SARS-CoV-2 replication, results showed no significant antiviral activity at concentrations up to 200 µM. Sci Rep. 2021 Mar 8;11(1):5433.
Human lung A549 cells 0.01–200 µM 72 hours Test the inhibitory effect of ML188 on SARS-CoV-2 replication, results showed no inhibition Sci Rep. 2021 Mar 8;11(1):5433
Vero E6 cells 0.01–200 µM 72 hours Test the inhibitory effect of ML188 on SARS-CoV-2 replication, results showed no inhibition Sci Rep. 2021 Mar 8;11(1):5433

Famotidine/法莫替丁 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice LPS-induced cytokine storm model Intraperitoneal injection (IP) 0.4 or 4 mg/kg Single injection or twice daily for 3 days To evaluate the inhibitory effect of famotidine on LPS-induced cytokine storm, results showed that famotidine significantly reduced serum and splenic TNF and IL-6 levels and improved survival rate. Mol Med. 2022 May 16;28(1):57.

Famotidine/法莫替丁 参考文献

[1]Inan A, Sen M, et al. Effects of the histamine H2 receptor antagonist famotidine on the healing of colonic anastomosis in rats. Clinics (Sao Paulo). 2009;64(6):567-70.

[2]Balcomb CC, Heller MC, Chigerwe M, Knych HK, Meyer AM. Pharmacokinetics and efficacy of intravenous famotidine in adult cattle. J Vet Intern Med. 2018 May;32(3):1283-1289

[3]Tolbert MK, Graham A, Odunayo A, Price J, Steiner JM, Newkirk K, Hecht S. Repeated Famotidine Administration Results in a Diminished Effect on Intragastric pH in Dogs. J Vet Intern Med. 2017 Jan;31(1):117-123

[4]Hedges K, Odunayo A, Price JM, Hecht S, Tolbert MK. Evaluation of the effect of a famotidine continuous rate infusion on intragastric pH in healthy dogs. J Vet Intern Med. 2019 Sep;33(5):1988-1994

[5]Golly E, Odunayo A, Daves M, Vose J, Price J, Hecht S, Steiner JM, Hillsman S, Tolbert MK. The frequency of oral famotidine administration influences its effect on gastric pH in cats over time. J Vet Intern Med. 2019 Mar;33(2):544-550

Famotidine/法莫替丁 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.96mL

0.59mL

0.30mL

14.82mL

2.96mL

1.48mL

29.63mL

5.93mL

2.96mL

Famotidine/法莫替丁 技术信息

CAS号76824-35-6
分子式C8H15N7O2S3
分子量 337.44
SMILES Code N=C(NS(=O)(N)=O)CCSCC1=CSC(NC(N)=N)=N1
MDL No. MFCD00079297
别名 MK-208; YM-11170; Famotidine, Famotidine Hydrochloride, MK-208, Pepcid, YM-11170, YM11170, YM 11170, MK 208, MK208
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

DMSO: 105 mg/mL(311.17 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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在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
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