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Chemical Structure| 34580-14-8 Chemical Structure| 34580-14-8

Structure of Ketotifen fumarate salt
CAS No.: 34580-14-8

Chemical Structure| 34580-14-8

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

Synonyms: Ketotifen fumarate; HC 20511 fumarate; HC 20511

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Product Details of Ketotifen fumarate salt

CAS No. :34580-14-8
Formula : C23H23NO5S
M.W : 425.50
SMILES Code : O=C(C1=C2C=CS1)CC3=CC=CC=C3C2=C4CCN(C)CC4.O=C(O)/C=C/C(O)=O
Synonyms :
Ketotifen fumarate; HC 20511 fumarate; HC 20511
MDL No. :MFCD00079394
InChI Key :YNQQEYBLVYAWNX-WLHGVMLRSA-N
Pubchem ID :5282408

Safety of Ketotifen fumarate salt

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P501-P270-P264-P301+P312+P330

Related Pathways of Ketotifen fumarate salt

GPCR

Isoform Comparison

Biological Activity

Target
  • H1 receptor

In Vitro:

Cell Line
Concentration Treated Time Description References
MC/9 mast cells 100 µg/mL 24 hours To evaluate the inhibitory effect of ketotifen on mast cell degranulation, results showed that ketotifen inhibited degranulation in a dose-dependent manner, with 100 µg/mL concentration reducing β-hexosaminidase release by more than 50%. Clin Cancer Res. 2024 Jun 3;30(11):2582-2597

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6OlaHsd mice Fibrosarcoma and osteosarcoma models Intraperitoneal injection 10 mg/kg Once daily for 8 days To evaluate the effect of ketotifen on tumor stiffness and vascular perfusion, results showed that 10 mg/kg dose significantly reduced tumor stiffness and improved vascular perfusion. Clin Cancer Res. 2024 Jun 3;30(11):2582-2597
New Zealand white rabbits Acidified pepsin-induced oesophagitis model Intravenous injection 0.05 mg/kg Administered 10 minutes before and during the exposure period Ketotifen significantly reduced acidified pepsin-induced oesophageal mucosal damage and inflammatory cell infiltration. Gut. 1997 Feb;40(2):175-81
Hens OPIDN model Oral 100 mg/kg Daily for 21 days To evaluate the protective effects of ketotifen against OPIDN, results showed it significantly alleviated TOCP-induced symptoms. Cell Discov. 2017 Aug 1;3:17024
Mice NMO model Oral 50 μM 1 day prior to and during the 3-day infusion To investigate the effect of ketotifen fumarate salt on NMO lesions. Results showed that ketotifen fumarate salt significantly reduced lesion severity and eosinophil infiltration. J Clin Invest. 2013 May;123(5):2306-16
Mice Laser-induced choroidal neovascularization model Intraperitoneal injection 25 mg/kg Starting 48 h before laser burn and continued daily until the day before sacrifice To assess the effect of mast cell stabilizer on choroidal neovascularization, results showed ketotifen fumarate significantly reduced CNV lesion size J Neuroinflammation. 2024 Oct 1;21(1):247
Mice Early life adversity model (NMSEW) Intraperitoneal injection 20 mg/kg 30 min before each adult stress episode, for 3 consecutive days Ketotifen prevented stress-induced reductions in sucrose preference and increases in cma1 expression in NMSEW females, but facilitated stress-induced sucrose anhedonia in NMSEW males and NH females. Brain Behav Immun. 2022 Jul;103:73-84
Guinea pigs Airway inflammation model Intraperitoneal injection 2 mg/kg Single dose, 30 minutes before mrIL-5 treatment To investigate the effect of ketotifen fumarate salt on mrIL-5-induced airway inflammation. Results showed that ketotifen reduced the mrIL-5-induced increase in eosinophils, neutrophils, and epithelial cells. Br J Pharmacol. 1992 Jan;105(1):19-22
Apoe−/− mice Chronic allergic lung inflammation and atherosclerosis model Nebulization 70 mg/5 mL Daily for 3 months To evaluate the therapeutic effects of ketotifen fumarate salt on chronic allergic lung inflammation and atherosclerosis. Results showed that ketotifen significantly reduced aortic arch lesion CD4+ and CD8+ T cells, mast cells, media SMC loss, lesion cell proliferation, angiogenesis, and apoptosis. Transl Res. 2016 May;171:1-16

Protocol

Bio Calculators
Preparing Stock Solutions 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

References

 

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