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Ketotifen fumarate salt

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Chemical Structure| 34580-14-8 同义名 : 酮替芬延胡索酸 ;Ketotifen fumarate;HC 20511 fumarate;HC 20511;Ketotifen (fumarate)
CAS号 : 34580-14-8
货号 : A208651
分子式 : C23H23NO5S
纯度 : 95%
分子量 : 425.497
MDL号 : MFCD00079394
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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

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].
实验方案
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
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