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
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)
|Body Surface Area (m2)||0.6||0.5||0.24||0.15||0.05||0.025||0.02||0.007|
|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|
Download Olopatadine HCl SDF
|Molecular Weight (MW)||373.87|
|Storage||3 years -20℃Powder|
|6 months-80℃in solvent (DMSO, water, etc.)|
|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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