Size | Price | Stock | Qty |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Rupatadine (also known as UR-12592) is a potent inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively. Rupatadine inhibits the effects of platelet-activating factor (PAF) and histamine (H1) by interacting with specific receptors. Rupatadine competitively suppresses histamine-induced guinea pig ileum contraction (pA2 = 9.29 ± 0.06) without affecting contraction induced by ACh, serotonin, or leukotriene D4 (LTD4). Additionally, it selectively prevents platelet aggregation caused by PAF in washed rabbit platelets (WRP) (pA2 = 6.68 ± 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 μM), but not in platelet aggregation caused by arachidonic acid or ADP.
Targets |
H1 Receptor ( Ki = 0.1 μM ); PAF ( Ki = 0.55 μM )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
In 0.5 ml of 50 mM PBS, pH 7.5, antagonists are incubated for 30 minutes at 25 °C with guinea pig cerebellum membranes (0.6 mg/ml) and [3H]-pyrilamine (1.2 nM). The incubation is ended by the addition of 5 ml of ice-cold PBS containing 2 μM pyrilamine and the collection of membranes on Whatman GF/B filters. After being cleaned with 3 × 5 ml of ice-cold PBS and 2 μM pyrilamine, the filters are placed in counting vials. Using 3 ml of HiSafe 3, liquid scintillation counting is used to determine the amount of radioactivity retained by each filter. The determination of specific binding is based on the variation in the amount of [3H]-pyrilamine bound when unlabeled promethazine (10 μM) is present compared to when it is not.
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Cell Assay |
C18-PAF is used to induce platelet aggregation, which is then measured with a dual-channel aggregometer Chrono-log 560. Platelet aggregation is measured both with and without the test compounds (5-min incubation). The inhibitors' activity is represented by their IC50 values. Rupatadine is tested in WRP against other aggregating agents, such as arachidonic acid (1 mM) and ADP (5 μM), in order to determine its selectivity. Rupatadine is present at different concentrations (3 × 10-7–3 × 10-5 M) and in the absence to obtain dose-response curves for PAF-induced aggregation in WRP.
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Animal Protocol |
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References |
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Molecular Formula |
C26H26CLN3
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Molecular Weight |
415.96
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Exact Mass |
415.18
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Elemental Analysis |
C, 75.08; H, 6.30; Cl, 8.52; N, 10.10
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CAS # |
158876-82-5
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Related CAS # |
Rupatadine Fumarate; 182349-12-8; Rupatadine-d4 fumarate; 1795153-63-7
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Appearance |
Solid powder
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SMILES |
CC1=CC(=CN=C1)CN2CCC(=C3C4=C(CCC5=C3N=CC=C5)C=C(C=C4)Cl)CC2
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InChi Key |
WUZYKBABMWJHDL-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C26H26ClN3/c1-18-13-19(16-28-15-18)17-30-11-8-20(9-12-30)25-24-7-6-23(27)14-22(24)5-4-21-3-2-10-29-26(21)25/h2-3,6-7,10,13-16H,4-5,8-9,11-12,17H2,1H3
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Chemical Name |
13-chloro-2-[1-[(5-methylpyridin-3-yl)methyl]piperidin-4-ylidene]-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaene
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4041 mL | 12.0204 mL | 24.0408 mL | |
5 mM | 0.4808 mL | 2.4041 mL | 4.8082 mL | |
10 mM | 0.2404 mL | 1.2020 mL | 2.4041 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03770923 | Recruiting | Drug: Rupatadine Drug: Montelukast |
Rheumatoid Arthritis | Sherief Abd-Elsalam | October 1, 2018 | Phase 3 |
NCT01481909 | Completed | Drug: Rupatadin | Mastocytosis | Marcus Maurer | September 2010 | Phase 2 Phase 3 |
NCT05356143 | Completed | Drug: Rupatadine | Healthy | J. Uriach and Company | December 2, 2021 | Phase 1 |
NCT01605487 | Completed | Drug: Rupatadine | Cold Contact Urticaria | Charite University, Berlin, Germany |
June 2012 | Phase 2 |
NCT01481909 | Completed | Drug: Rupatadin | Mastocytosis | Marcus Maurer | September 2010 | Phase 2 Phase 3 |