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/ Ketotifen fumarate salt

富马酸酮替芬 /Ketotifen fumarate salt {[allProObj[0].p_purity_real_show]}

货号：A208651 同义名： 酮替芬延胡索酸 / Ketotifen fumarate;HC 20511 fumarate

Ketotifen fumarate is a noncompetitive H1 receptor antagonist and mast cell stabilizer that is used to treat asthma.

Ketotifen fumarate salt 化学结构 CAS号：34580-14-8
Ketotifen fumarate salt 化学结构
CAS号：34580-14-8
Ketotifen fumarate salt 3D分子结构
CAS号：34580-14-8
Ketotifen fumarate salt 化学结构 CAS号：34580-14-8
Ketotifen fumarate salt 3D分子结构 CAS号：34580-14-8
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Ketotifen fumarate salt 纯度/质量文件 产品仅供科研

货号：A208651 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。

Ketotifen fumarate salt 生物活性

靶点

  • H1 receptor
描述 Ketotifen fumarate blocks histamine1 (H1) receptors, stabilizes mast cells, and acts as an eosinophil inhibitor (decreases chemotaxis and activation of eosinophils). Ketotifen was safe and statistically effective in reducing ocular itching and hyperemia associated with allergic conjunctivitis. Ketotifen's rapid onset of action (within 15 minutes) and extended duration of action (at least 8 hours) make it a valuable treatment for allergic conjunctivitis[3]. Ketotifen is an orally active prophylactic agent for the management of bronchial asthma and allergic disorders. Unlike inhaled sodium cromoglycate, ketotifen ameliorates the symptoms of asthma, rhinitis and dermatitis when present together in atopic patients[4]. Subgroups of animals were treated twice daily for one week with or without ketotifen fumarate (5 mg/kg). Ketotifen fumarate attenuated the initiation and progression of gingivitis and reduced the oxidative stress, and inhibited NF-κB and p38 MAPK related with mast cells and macrophages accumulation[5]. In EAO (experimental autoimmune orchitis) model, KF significantly reduced severity of histopathological testicular damage compared to rats in the vehicle group. KF also reduced the number of testicular MC (Mast cells) compared to vehicle group[6].

Ketotifen fumarate salt 参考文献

[1]Wada Y, Ami S, et al. Generic selection criteria for safety and patient benefit [V] : Comparing the pharmaceutical properties and patient usability of original and generic nasal spray containing ketotifen fumarate. Drug Discov Ther. 2016;10(2):88-92.

[2]Klooker TK, Braak B, et al. The mast cell stabiliser ketotifen decreases visceral hypersensitivity and improves intestinal symptoms in patients with irritable bowel syndrome. Gut. 2010 Sep;59(9):1213-21.

[3]Abelson MB, Chapin MJ, Kapik BM, Shams NB. Efficacy of ketotifen fumarate 0.025% ophthalmic solution compared with placebo in the conjunctival allergen challenge model. Arch Ophthalmol. 2003 May;121(5):626-30

[4]Grant SM, Goa KL, Fitton A, Sorkin EM. Ketotifen. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in asthma and allergic disorders. Drugs. 1990 Sep;40(3):412-48

[5]Yuan W, Hou S, Jia H, Qiu Z, Liu T, Chen X, Li H, Sun Y, Liang L, Sui X, Zhao X, Zhao Z. Ketotifen fumarate attenuates feline gingivitis related with gingival microenvironment modulation. Int Immunopharmacol. 2018 Dec;65:159-173

[6]Moreno D, Sobarzo CM, Lustig L, Rodríguez Peña MG, Guazzone VA. Effect of ketotifen fumarate on experimental autoimmune orchitis and torsion of the spermatic cord. Asian J Androl. 2020 Jan-Feb;22(1):112-117

Ketotifen fumarate salt 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.24mL

11.75mL

2.35mL

1.18mL

23.50mL

4.70mL

2.35mL

Ketotifen fumarate salt 技术信息

CAS号34580-14-8
分子式C23H23NO5S
分子量 425.497
别名 酮替芬延胡索酸 ;Ketotifen fumarate;HC 20511 fumarate;HC 20511;Ketotifen (fumarate)
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 105 mg/mL(246.77 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

H2O: 15 mg/mL(35.25 mM)，配合低频超声助溶
动物实验配方

5% DMSO+45% PEG 300+water 16 mg/mL

Tags: Ketotifen | 34580-14-8 | HC 20511 | HC20511 | HC-20511 | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Metabolic Enzyme/Protease | Anti-infection | Histamine Receptor | Endogenous Metabolite | SARS-CoV | Influenza Virus | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Ketotifen fumarate salt 纯度/质量文件 | Ketotifen fumarate salt 亚型比较 | Ketotifen fumarate salt 生物活性 | Ketotifen fumarate salt 参考文献 | Ketotifen fumarate salt 实验方案 | Ketotifen fumarate salt 技术信息

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