Structure of Ketotifen fumarate salt
CAS No.: 34580-14-8
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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
4.5
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Batch number can be found on the product's label following the word 'Batch'.
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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 |
GHS Pictogram: |
![]() |
Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P501-P270-P264-P301+P312+P330 |
Target |
|
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 |
Bio Calculators | ||||
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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 |
Tags: Ketotifen | HC 20511 | HC20511 | HC-20511 | Histamine Receptor | Endogenous Metabolite | SARS-CoV | Influenza Virus | SARS coronavirus | mast cell | antiviral | PR8 | pH1N1 | H3N2 | encephalomyelitis | asthma | inhibitor | 34580-14-8 |
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Code | Phrase |
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P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
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P304 + P312 | IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell. |
P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
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P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
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P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
P333 + P313 | IF SKIN irritation or rash occurs: Get medical advice/attention. |
P335 + P334 | Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages. |
P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
P370 + P376 | In case of fire: Stop leak if safe to Do so. |
P370 + P378 | In case of fire: |
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Storage | |
Code | Phrase |
P401 | |
P402 | Store in a dry place. |
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P410 + P412 | Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF. |
P411 + P235 | Keep cool. |
Disposal | |
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H240 | Heating may cause an explosion |
H241 | Heating may cause a fire or explosion |
H242 | Heating may cause a fire |
H250 | Catches fire spontaneously if exposed to air |
H251 | Self-heating; may catch fire |
H252 | Self-heating in large quantities; may catch fire |
H260 | In contact with water releases flammable gases which may ignite spontaneously |
H261 | In contact with water releases flammable gas |
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H272 | May intensify fire; oxidizer |
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H290 | May be corrosive to metals |
Health hazards | |
Code | Phrase |
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H301 | Toxic if swallowed |
H302 | Harmful if swallowed |
H303 | May be harmful if swallowed |
H304 | May be fatal if swallowed and enters airways |
H305 | May be harmful if swallowed and enters airways |
H310 | Fatal in contact with skin |
H311 | Toxic in contact with skin |
H312 | Harmful in contact with skin |
H313 | May be harmful in contact with skin |
H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
H317 | May cause an allergic skin reaction |
H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
H330 | Fatal if inhaled |
H331 | Toxic if inhaled |
H332 | Harmful if inhaled |
H333 | May be harmful if inhaled |
H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
H341 | Suspected of causing genetic defects |
H350 | May cause cancer |
H351 | Suspected of causing cancer |
H360 | May damage fertility or the unborn child |
H361 | Suspected of damaging fertility or the unborn child |
H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
H370 | Causes damage to organs |
H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
Code | Phrase |
H400 | Very toxic to aquatic life |
H401 | Toxic to aquatic life |
H402 | Harmful to aquatic life |
H410 | Very toxic to aquatic life with long-lasting effects |
H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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