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Chemical Structure| 90729-43-4 Chemical Structure| 90729-43-4

Structure of Ebastine
CAS No.: 90729-43-4

Chemical Structure| 90729-43-4

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Ebastine is a selective H1-histamine receptor antagonist.

Synonyms: LAS-W 090; RP64305; Kestin

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Product Details of Ebastine

CAS No. :90729-43-4
Formula : C32H39NO2
M.W : 469.66
SMILES Code : O=C(C1=CC=C(C(C)(C)C)C=C1)CCCN2CCC(OC(C3=CC=CC=C3)C4=CC=CC=C4)CC2
Synonyms :
LAS-W 090; RP64305; Kestin
MDL No. :MFCD00865661
InChI Key :MJJALKDDGIKVBE-UHFFFAOYSA-N
Pubchem ID :3191

Safety of Ebastine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H413
Precautionary Statements:P264-P270-P273-P301+P312-P330

Related Pathways of Ebastine

GPCR

Isoform Comparison

Biological Activity

Target
  • H1 receptor

In Vitro:

Cell Line
Concentration Treated Time Description References
U2OS cells 15.505 µM 48 h Ebastine significantly inhibited the growth of U2OS cells and induced cell cycle arrest and apoptosis. PMC9830506
MG63 cells 13.254 µM 48 h Ebastine significantly inhibited the growth of MG63 cells and induced cell cycle arrest and apoptosis. PMC9830506
MNNG cells 13.635 µM 48 h Ebastine significantly inhibited the growth of MNNG cells and induced cell cycle arrest and apoptosis. PMC9830506
Rat isolated heart 605.7 to 383.3 ng·mL⁻¹ 130 min To investigate the pharmacokinetics of ebastine in rat heart, showing that ebastine was metabolized to hydroxyebastine and further to carebastine. PMC3166699
NIH/3T3 cells 0.01-40 μM 48 h Evaluate the sensitivity of EBA to normal cells, showing higher sensitivity to TNBC cells than normal cells PMC10130003
4T1 cells 0-40 μM 24-48 h Evaluate the effect of EBA on TNBC cell viability, showing concentration-dependent reductions in cell viability PMC10130003
BT549 cells 0-40 μM 24-48 h Evaluate the effect of EBA on TNBC cell viability, showing concentration-dependent reductions in cell viability PMC10130003
MDA-MB-231 cells 0-40 μM 24-48 h Evaluate the effect of EBA on TNBC cell viability, showing concentration-dependent reductions in cell viability PMC10130003
HepG2 cells 5 or 10 μM 16 or 24 h To investigate the effect of ebastine on MKRN1 protein levels, results showed that ebastine decreased MKRN1 protein levels, which was reversed by the proteasome inhibitor MG132. PMC11785899
LAD2 human mast cells 3 μg/mL 20 h To study the inhibitory effect of ebastine on MC degranulation, results showed ebastine significantly reduced the induction of inflammatory factors by MC degranulation PMC11074640

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Subcutaneous transplantation model and lung metastasis model Oral 0.5 mg/day and 1 mg/day Once daily for 30/45 days Ebastine significantly inhibited tumor growth and lung metastasis, with no obvious toxic effects observed. PMC9830506
Wistar rats Isolated heart perfusion model Perfusion 7.8 to 12.1 mg Single dose, 130 minutes duration To evaluate the pharmacokinetics and negative inotropic effect of ebastine in rat heart, showing metabolism to hydroxyebastine and carebastine with significant negative inotropic effects. PMC3166699
Guinea pigs Arrhythmogenicity model Oral 20 mg/kg Single dose, recorded for 4 hours Evaluate the effect of ketoconazole on Ebastine-induced QTc interval prolongation; results showed Ebastine did not further prolong QTc interval after ketoconazole pretreatment PMC1915872
BALB/c mice BCSC-enriched 4T1 allograft model Intraperitoneal injection 20 mg/kg Every other day for 34 days Evaluate the effect of EBA on BCSC-enriched tumor growth, showing significant inhibition of tumor growth and metastasis PMC10130003
Mice High-fat-high-fructose diet (HFHFD)-induced MASH model Intraperitoneal injection 1 and 5 mg/kg Daily injections for 4 weeks To investigate the protective effect of ebastine on HFHFD-induced MASH, results showed that ebastine significantly reduced the risk of MASH, with a decrease in MKRN1 expression and an increase in AMPK activity. PMC11785899
CB17SCID mice Triple-negative breast cancer (SUM159) xenograft model Oral 30 mg/kg 5 days per week, for about 28 days To evaluate the effect of ebastine on tumor growth and progression in triple-negative breast cancer PMC7541747
C57BL/6N-ACE2em2(hACE2-WPRE, pgk-puro)/CCLA mice SARS-CoV-2 infection model Intraperitoneal injection 5 mg/kg Daily administration, continued until 5 days post-infection To study the protective effect of ebastine on SARS-CoV-2-induced tracheal injury, results showed ebastine significantly reduced MC degranulation and tracheal injury PMC11074640

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01144832 Irritable Bowel Syndrome Phase 4 Completed - Belgium ... More >> University hospitals Leuven Leuven, Vlaams-Brabant, Belgium, 3000 Less <<
NCT01940393 Urticaria Phase 4 Completed - Colombia ... More >> Medellin Medellin, Antioquia, Colombia Less <<
NCT02065440 Cough Not Applicable Unknown - Korea, Republic of ... More >> Division of Pulmonary and Critical Care Medicine, Department of Internal Medicine, Seoul Metropolitan Government, Seoul National University Boramae Medical Center Seoul, Dongjak-Gu, Korea, Republic of, 156-707 Less <<
NCT01908465 Irritable Bowel Syndrome (IBS) Phase 4 Recruiting March 2018 Belgium ... More >> UZ Antwerpen Not yet recruiting Edegem, Antwerpen, Belgium, 2650 Contact: Tom Moreels, M.D.    +32 3 821 33 24    tom.moreels@uza.be    Sub-Investigator: Tom Moreels, M.D.          ZOL (Ziekenhuis Oost-Limburg) Recruiting Genk, Limburg, Belgium, 3600 Contact: Philip Caenepeel, M.D.    +32 8 32 65 13    philip.caenepeel@zol.be    Sub-Investigator: Philip Caenepeel, M.D.          UZ Gent Recruiting Gent, Oost-Vlaanderen, Belgium, 9000 Contact: Sabine Van de Moortele    +32 9 332 68 54    Sabine.VandeMoortele@uzgent.be    Contact: Muriël Fouquet    +32 9 332 33 36    Muriel.Fouquet@uzgent.be    Sub-Investigator: Danny De Looze, M.D.          AZ Sint-Elizabeth Zottegem Recruiting Zottegem, Oost-Vlaanderen, Belgium, 9620 Contact: Inge Vanslembrouck, M.D.    +32 93 64 83 41    inge.vanslembrouck@sezz.be    Contact: Inge Vanslembrouck, M.D.    +32 93 64 83 43    inge.vanslembrouck@sezz.be    Sub-Investigator: Sebastien Kindt, M.D.          UZ Leuven Recruiting Leuven, Vlaams-Brabant, Belgium, 3000 Contact: Lien Beullens, MSc    0032-16-341943    lien.beullens@kuleuven.be    Contact: Dafne Balemans    0032-16-330158    dafne.balemans@med.kuleuven.be    Principal Investigator: Guy Boeckxstaens, M.D.          AZ Sint-Lucas Brugge Recruiting Brugge, West-Vlaanderen, Belgium, 8310 Contact: Hilde Nevens    +32 50 36 57 11    hilde.nevens@stlucas.be    Contact: Joris Arts, M.D.    +32 50 36 51 55    jar@stlucas.be    Sub-Investigator: Joris Arts, M.D.          Netherlands Rijnstate Not yet recruiting Arnhem, Gelderland, Netherlands, 6800 Contact: B.G. Baten, M.D.    0031 88 005 6671       Contact: D. Hirsch, M.D.       DHirsch@Rijnstate.nl    Sub-Investigator: D. Hirsch, M.D.          Medisch Spectrum Twente Not yet recruiting Enschede, Limburg, Netherlands, 7500 Contact: Anita Westerhof    0031(53)4877511       Contact: J. Kolkman, M.D.    0031 (53) 487 24 10    j.kolkman@mst.nll    Sub-Investigator: J. Kolkman, M.D.          AZ Maastricht Not yet recruiting Maastricht, Limburg, Netherlands, 6202 Contact: Samefko Ludidi          Contact: A. Masclee, M.D.       a.masclee@mumc.nl    Sub-Investigator: A. Masclee          Sint Lucas Andreas Ziekenhuis Not yet recruiting Amsterdam, Noord-Holland, Netherlands, 1061 Contact: Sjoerd Kuiken, M.D.       s.kuiken@slaz.nl    Sub-Investigator: Sjoerd Kuiken, M.D.          Academisch Medisch Centrum Not yet recruiting Amsterdam, Noord-Holland, Netherlands, 1105 Contact: A.J. Bredenoord, M.D.       A.J.Bredenoord@amc.uva.nl    Sub-Investigator: A.J. Bredenoord, M.D.          Tergooiziekenuizen Blaricum/Hilversum Not yet recruiting Hilversum/Blaricum, Noord-Holland, Netherlands, 1213/1261 Contact: Karen Verloop    0031 (35) 539 19 25    kverloop@tergooiziekenhuizen.nl    Contact: B. van den Elzen, M.D.       BvandenElzen@tergooiziekenhuizen.nl    Sub-Investigator: B. van den Elzen, M.D. Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.06mL

21.29mL

4.26mL

2.13mL

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