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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 Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $30 | In Stock | |
25 mg | $52 | In Stock | |
50 mg | $87 | In Stock | |
100 mg | $135 | In Stock |
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]. |
Alias | UR-12592, UR12592 |
Molecular Weight | 415.96 |
Formula | C26H26ClN3 |
Cas No. | 158876-82-5 |
Smiles | ClC=1C=CC2=C(C1)CCC=3C=CC=NC3C2=C4CCN(CC=5C=NC=C(C5)C)CC4 |
Storage | keep 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
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