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Emedastine

Emedastine
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Purity:97.1%
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Emedastine

Catalog No. T3979Cas No. 87233-61-2
Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.
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Pack SizePriceAvailabilityQuantity
1 mg$31In Stock
5 mg$72In Stock
10 mg$117In Stock
25 mg$197In Stock
50 mg$293In Stock
100 mg$437In Stock
500 mg$982In Stock
1 mL x 10 mM (in DMSO)$79In Stock
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Product Introduction

Bioactivity
Description
Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.
Targets&IC50
H1 receptor:1.3 nM(Ki)
AliasLY188695, Emadine
Chemical Properties
Molecular Weight302.41
FormulaC17H26N4O
Cas No.87233-61-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (165.33 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.3068 mL16.5338 mL33.0677 mL165.3384 mL
5 mM0.6614 mL3.3068 mL6.6135 mL33.0677 mL
10 mM0.3307 mL1.6534 mL3.3068 mL16.5338 mL
20 mM0.1653 mL0.8267 mL1.6534 mL8.2669 mL
50 mM0.0661 mL0.3307 mL0.6614 mL3.3068 mL
100 mM0.0331 mL0.1653 mL0.3307 mL1.6534 mL

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