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140462-76-6 (Olopatadine (hydrochloride))

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Identification

Olopatadine (hydrochloride) Olopatadine (hydrochloride)
Name Olopatadine (hydrochloride)
Formula C21H24ClNO3
MW 373.87
CAS No. 140462-76-6
EINECS
Smiles O=C(O)CC1=CC=C(C/2=C1)OCC3=CC=CC=C3C2=CCCN(C)C.[H]Cl
Synonyms (Z)-11-[3-(Dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride; (Z)-2-(11-(3-(dimethylamino)propylidene)-6,11-dihydrodibenzo[b,e]oxepin-2-yl)acetic acid hydrochloride
InChI InChI=1S/C21H23NO3.ClH/c1-22(2)11-5-8-18-17-7-4-3-6-16(17)14-25-20-10-9-15(12-19(18)20)13-21(23)24;/h3-4,6-10,12H,5,11,13-14H2,1-2H3,(H,23,24);1H/b18-8-;
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Introduction

Olopatadine HCl is a histamine blocker used to treat allergic conjunctivitis. Target: Histamine Receptor Olopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders.

Background Information

Olopatadine hydrochloride (Opatanol) is a histamine blocker and mast cell stabilizer with an IC50 of 559 uM for the release of histamine. Evaluation of the interaction of olopatadine with histamine receptors revealed a relatively high affinity for the H1 receptor (Ki = 31.6 nM, pKi = 7.5 ?0.1) but lower affinities for H2 receptors (Ki = 100 uM, pKi = 4.0 ?0.19) and H3 receptors (Ki = 79.4 uM, pKi = 4.1 ?0.16,). The H1 selectivity of olopatadine was superior to that of other ocularly used anti-histamines studied, such as ketotifen, levocabastine, antazoline and pheniramine. ......by AbMole BioScience
Olopatadine hydrochloride is a dual acting histamine H1-receptor antagonist and mast cell stabilizer ......by AdooQ BioScience, LLC
Olopatadine HCl is a histamine blocker and mast cell stabilizer with an IC50 of 559 μM for the release of histamine ......by BOC Sciences
Olopatadine HCl is a relatively selective histamine H1 antagonist. It acts by inhibiting histamine induced effects on human conjunctival epithelial cells. ......by MedKoo Biosciences, Inc.
Olopatadine HCl is a histamine blocker used to treat allergic conjunctivitis. Olopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. ......by Target Molecule Corp.
Histamine H1 receptor antagonist (Ki = 31.6 nM). Inhibits the release of histamine, prostaglandin D2 and tryptase in a concentration-dependent manner. Mast cell stabilizer; inhibits mast cell mediator release. Also suppresses inflammation by inhibition of cytokine production. ......by Tocris Bioscience Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000012354

Storage condition

Desiccate at RT by Tocris Bioscience Inc.

Solubility

DMSO 75 mg/mL; Water 15 mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 75 mg/mL (200.6 mM); Water13 mg/mL (34.77 mM); Ethanol8 mg/mL (21.39 mM) by Selleck Chemicals LLC
Soluble to 75 mM in water and to 100 mM in DMSO by Tocris Bioscience Inc.
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Mechanism and Indication

Signaling Pathways Immunology/Inflammation GPCR/G Protein
Target Histamine Receptor
Research Area Inflammation/Immunology
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Olopatadine (hydrochloride) - Launched
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Safety Data of Olopatadine (hydrochloride)

Hazard Symbols : T,N
Risk Statements : 25-50
Safety Statements : 45-61
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Spectral Information

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Suppliers List

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Related Products

Other Forms of 140462-76-6

Name CAS No Formula MW

Recommended Compounds in Histamine Receptor

Name CAS No Formula MW
Doxylamine (succinate) 562-10-7 C21H28N2O5 388.46
Ebastine 90729-43-4 C32H39NO2 469.66
Azelastine 58581-89-8 C22H24ClN3O 381.9
Epinastine 80012-43-7 C16H15N3 249.31
Hydroxyzine (dihydrochloride) 2192-20-3 C21H29Cl3N2O2 447.83
Hydroxyzine 68-88-2 C21H27ClN2O2 374.9
Desloratadine 100643-71-8 C19H19ClN2 310.82
Pemirolast (potassium) 100299-08-9 C10H7KN6O 266.3
Betahistine (dihydrochloride) 5579-84-0 C8H14Cl2N2 209.12
Brompheniramine (maleate) 980-71-2 C20H23BrN2O4 435.31
Azelastine (hydrochloride) 79307-93-0 C22H25Cl2N3O 418.36
Famotidine 76824-35-6 C8H15N7O2S3 337.45
Meclizine (dihydrochloride) 1104-22-9 C25H29Cl3N2 463.87
Nizatidine 76963-41-2 C12H21N5O2S2 331.46
Roxatidine (Acetate Hydrochloride) 93793-83-0 C19H29ClN2O4 384.9
Diphenhydramine (hydrochloride) 147-24-0 C17H22ClNO 291.82
Clemastine (fumarate) 14976-57-9 C25H30ClNO5 459.96
Chlorpheniramine (maleate) 113-92-8 C20H23ClN2O4 390.86
Ranitidine (hydrochloride) 66357-59-3 C13H23ClN4O3S 350.86
Mianserin (hydrochloride) 21535-47-7 C18H21ClN2 300.83

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

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More Information

Olopatadine (hydrochloride)

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