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Chemical Structure| 190786-44-8 Chemical Structure| 190786-44-8

Structure of Bepotastine besilate
CAS No.: 190786-44-8

Chemical Structure| 190786-44-8

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Bepotastine besilate is a selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.

Synonyms: Bepotastine(besylate); TAU 284; Bepotastine(besilate)

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Product Details of Bepotastine besilate

CAS No. :190786-44-8
Formula : C27H31ClN2O6S
M.W : 547.06
SMILES Code : O=C(O)CCCN1CCC(O[C@@H](C2=CC=C(Cl)C=C2)C3=NC=CC=C3)CC1.O=S(C4=CC=CC=C4)(O)=O
Synonyms :
Bepotastine(besylate); TAU 284; Bepotastine(besilate)
MDL No. :MFCD01938491
InChI Key :UDGHXQPQKQPSBB-BOXHHOBZSA-N
Pubchem ID :164521

Safety of Bepotastine besilate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Bepotastine besilate

GPCR

Isoform Comparison

Biological Activity

Target
  • H1 receptor

    Histamine H1 receptor, pIC50:5.7

In Vitro:

Cell Line
Concentration Treated Time Description References
Human primary NK cells 20 μM 24 h To evaluate the inhibitory effect of Bepotastine on influenza virus replication, results showed that Bepotastine effectively inhibited viral replication PMC11321118
Human primary alveolar epithelial cells 20 μM 24 h To evaluate the inhibitory effect of Bepotastine on influenza virus replication, results showed that Bepotastine effectively inhibited viral replication PMC11321118
MDCK cells 5, 10, 20 μM 24 h To evaluate the inhibitory effect of Bepotastine on influenza virus replication, results showed that Bepotastine effectively inhibited viral replication PMC11321118
A549 cells 5, 10, 20 μM 24 h To evaluate the inhibitory effect of Bepotastine on influenza virus replication, results showed that Bepotastine effectively inhibited viral replication PMC11321118

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice Influenza virus infection model Intraperitoneal injection 2, 10, 50 mg/kg Once daily from day –5 to day 10 To evaluate the protective effect of Bepotastine against influenza virus infection, results showed that Bepotastine alleviated weight loss and improved survival rate PMC11321118
Mice Aged mouse model of mechanical alloknesis Oral 3 mg/kg Single administration Evaluate the effect of Bepotastine on mechanical alloknesis in aged mice, showing no significant suppression PMC11110811

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02686294 Rhinitis, Allergic, Perennial Phase 1 Completed - Korea, Republic of ... More >> The Korea Univertisy Anam Hospital Seoul, Korea, Republic of, 136-705 Less <<
NCT02682745 Rhinitis, Allergic, Perennial Phase 1 Completed - Korea, Republic of ... More >> The Korea Univertisy Anam Hospital Seoul, Korea, Republic of, 136-705 Less <<
NCT03200496 Healthy Phase 1 Completed - Korea, Republic of ... More >> Korea University Anam Hospital Seoul, Korea, Republic of Less <<
NCT01277341 Seasonal Allergic Rhinitis Phase 2 Completed - United States, California ... More >> ISTA Pharmaceuticals, Inc. Irvine, California, United States, 92618 Less <<
NCT01339507 - Completed - United States, Texas ... More >> Derek Cunningham Austin, Texas, United States, 78746 Less <<
NCT00586664 Allergic Conjunctivitis Phase 3 Completed - United States, California ... More >> ISTA Pharmaceuticals, Inc. Irvine, California, United States, 92618 Less <<
NCT01578278 Seasonal Allergic Rhinitis Phase 2 Completed - United States, California ... More >> ISTA Pharmaceuticals, Inc. Irvine, California, United States, 92618 Less <<
NCT00586625 Allergic Conjunctivitis Phase 3 Completed - -
NCT01174823 Allergic Conjunctivitis Phase 2 Completed - United States, California ... More >> ISTA Pharmaceuticals, Inc. Irvine, California, United States, 92618 Less <<
NCT00586664 - Completed - -
NCT01346371 Allergic Conjunctivitis Phase 4 Unknown August 2012 United States, Minnesota ... More >> Minnesota Eye Consultants, P.A. Minneapolis, Minnesota, United States, 55404 Less <<
NCT01222299 Allergic Rhinitis Phase 1 Phase 2 Completed - United States, California ... More >> ISTA Pharmaceuticals, Inc. Irvine, California, United States, 92618 Less <<
NCT00586625 - Completed - -
NCT02332044 Healthy Phase 1 Completed - -
NCT01897428 Allergic Rhinitis ... More >> Urticaria Pruritus Less << Phase 1 Completed - Korea, Republic of ... More >> Dept. of Clinical Pharmacology & Toxicology, Anam Hospital Seoul, Korea, Republic of, 136-705 Less <<
NCT01925313 Healthy Phase 1 Completed - Korea, Republic of ... More >> Yonsei university severance hospital Seoul, Korea, Republic of Less <<
NCT00424398 Conjunctivitis, Allergic Phase 2 Phase 3 Completed - United States, California ... More >> ISTA Pharmaceuticals, Inc. Irvine, California, United States, 92630 Less <<
NCT01425632 Perennial Allergic Rhinitis Phase 3 Completed - Japan ... More >> Reserch site Chubu, Japan Reserch site Hokuriku, Japan Reserch site Kanto, Japan Reserch site Kinki, Japan Reserch site Kyusyu, Japan Less <<
NCT01840605 Dermatitis At... More >>opic Less << Phase 3 Completed - Japan ... More >> Medical Corporation Kojinkai Asanuma Dermatology Clinic Hokkaido, Japan Less <<
NCT01425632 - Completed - -
NCT01840605 - Completed - -
NCT00424398 - Completed - -
NCT01128556 Histamine Responsive Allergy P... More >>atients Less << Phase 4 Completed - United States, Texas ... More >> North Texas Institute for Clinical Trials Fort Worth, Texas, United States, 76132 Less <<
NCT01450176 Eye Allergies Not Applicable Completed - United States, Tennessee ... More >> McCabe Vision Center Murfreesboro, Tennessee, United States, 37129 Less <<
NCT01753739 Seasonal Allergic Rhinitis Phase 2 Completed - United States, California ... More >> Bausch & Lomb Incorporated Irvine, California, United States, 92618-2301 Less <<
NCT01861522 Perennial Allergic Rhinitis Phase 3 Completed - Japan ... More >> Reserch site Fukuoka, Japan Reserch site Toyama, Japan Less <<
NCT01861522 - Completed - -
NCT01900054 Perennial Allergic Rhinitis PHASE3 COMPLETED 2025-11-13 Reserch site, Kanagawa, Japan
NCT01443442 Allergic Conjunctivitis Phase 4 Completed - United States, California ... More >> Eye Car Center, Southern California college of Optometry Fullerton, California, United States, 92831 Eye Care Center, Southern Caalifornia College of Optometry Fullerton, California, United States, 92831 Less <<
NCT01337557 Allergic Conjunctivitis Phase 4 Unknown November 2011 -
NCT01900054 Perennial Allergic Rhinitis PHASE3 COMPLETED 2025-11-13 Reserch site, Kanagawa, Japan

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.14mL

1.83mL

0.91mL

18.28mL

3.66mL

1.83mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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