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Olopatadine HCl 140462-76-6

Product Description

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Molecular Weight: 373.87 Olopatadine HCl is a histamine blocker and mast cell stabilizer with an IC50 of 559 μM for the release of histamine

Biological Activity

Olopatadine hydrochloride(Opatanol) is a histamine blocker and mast cell stabilizer with an IC50 of 559 µM 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 µM, pKi = 4.0 ± 0.19) and H3 receptors (Ki = 79.4 µM, 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.






Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by Animal B Km
Animal A Km



For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × mouse Km(3) = 11.2 mg/kg
rat Km(6)







Chemical Information

Download Olopatadine HCl SDF



Molecular Weight (MW) 373.87
Formula

C21H23NO3.HCl

CAS No. 140462-76-6

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms



Solubility (25°C) * In vitro DMSO 75 mg/mL (200.6 mM)
Water 13 mg/mL (34.77 mM)
Ethanol 8 mg/mL (21.39 mM)




Chemical Name (11Z)-11-[3-(dimethylamino)propylidene]-6,11-dihydro-dibenz[b,e]oxepin-2-acetic acid, hydrochloride (1:1)









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Product Categories : Neuronal Signaling > Histamine Receptor Inhibitor

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