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Rupatadine

🥰Excellent
Catalog No. T36618Cas No. 158876-82-5
Alias UR-12592, UR12592

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

Rupatadine

Rupatadine

🥰Excellent
Purity: 99.87%
Catalog No. T36618Alias UR-12592, UR12592Cas No. 158876-82-5
Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.
Pack SizePriceAvailabilityQuantity
10 mg$30In Stock
25 mg$52In Stock
50 mg$87In Stock
100 mg$135In Stock
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Purity:99.87%
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Product Introduction

Bioactivity
Description
Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.
Targets&IC50
PAF-induced platelet aggregation (human plasma):0.68 μM, H1 Receptor:0.1 μM (Ki), PAF:0.55 μM (Ki)
In vitro
Rupatadine acts as a dual H1 and PAF receptor antagonist. Rupatadine has a Ki of 0.10 μM for H1 and 0.55 μM for PAF receptors. Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA₂ = 9.29), and PAF-induced platelet aggregation in rabbit platelets (pA₂ = 6.68) and human plasma (IC₅₀ = 0.68 μM), without affecting ACh, 5-HT, or LTD₄ responses[1].
In vivo
Rupatadine blocks histamine- and PAF-induced hypotension (ID₅₀ = 1.4 and 0.44 mg/kg i.v.) and bronchoconstriction (113 and 9.6 μg/kg i.v.). Rupatadine protects mice from PAF- and endotoxin-induced death (ID₅₀ = 0.31-3.0 mg/kg). In dogs, 1 mg/kg p.o. still inhibited vascular permeability >26 h. No sedation was observed at 100 mg/kg[1].
AliasUR-12592, UR12592
Chemical Properties
Molecular Weight415.96
FormulaC26H26ClN3
Cas No.158876-82-5
SmilesClC=1C=CC2=C(C1)CCC=3C=CC=NC3C2=C4CCN(CC=5C=NC=C(C5)C)CC4
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 100 mg/mL (240.41 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4041 mL12.0204 mL24.0408 mL120.2039 mL
5 mM0.4808 mL2.4041 mL4.8082 mL24.0408 mL
10 mM0.2404 mL1.2020 mL2.4041 mL12.0204 mL
20 mM0.1202 mL0.6010 mL1.2020 mL6.0102 mL
50 mM0.0481 mL0.2404 mL0.4808 mL2.4041 mL
100 mM0.0240 mL0.1202 mL0.2404 mL1.2020 mL

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