Rupatadine FumarateCAS# 182349-12-8 |
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Quality Control & MSDS
3D structure
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| Cas No. | 182349-12-8 | SDF | Download SDF |
| PubChem ID | 6449107 | Appearance | Powder |
| Formula | C30H30ClN3O4 | M.Wt | 532.03 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 30 mg/mL (56.39 mM; Need ultrasonic and warming) | ||
| Chemical Name | (E)-but-2-enedioic acid;8-chloro-11-[1-[(5-methylpyridin-3-yl)methyl]piperidin-4-ylidene]-5,6-dihydrobenzo[1,2]cyclohepta[2,4-b]pyridine | ||
| SMILES | CC1=CC(=CN=C1)CN2CCC(=C3C4=C(CCC5=C3N=CC=C5)C=C(C=C4)Cl)CC2.C(=CC(=O)O)C(=O)O | ||
| Standard InChIKey | JYBLCDXVHQWMSU-WLHGVMLRSA-N | ||
| Standard InChI | InChI=1S/C26H26ClN3.C4H4O4/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;5-3(6)1-2-4(7)8/h2-3,6-7,10,13-16H,4-5,8-9,11-12,17H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+ | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).
IC50 value:
Target: PAF/H1 antagonist
in vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 microM), while not affecting ADP- or arachidonic acid-induced platelet aggregation [1]. The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7+/-0.4 microM, 3.2+/-0.7 microM and 1.5+/-0.4 microM, respectively whereas for loratadine the IC50 was 2.1+/-0.9 microM, 4.0+/-1.3 M and 1.7+/-0.5 microM. SR-27417A exhibited no inhibitory effect [2].
in vivo: Rupatadine blocked histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 micrograms/kg i.v.). Moreover, it potently inhibited PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg/kg i.v.) [1]. rupatadine treatment improved the declined lung function and significantly decreased animal death. Moreover, rupatadine was able not only to attenuate silica-induced silicosis but also to produce a superior therapeutic efficacy compared to pirfenidone, histamine H1 antagonist loratadine, or PAF antagonist CV-3988 [3]. References: | |||||
Rupatadine Fumarate Dilution Calculator
Rupatadine Fumarate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8796 mL | 9.398 mL | 18.7959 mL | 37.5919 mL | 46.9898 mL |
| 5 mM | 0.3759 mL | 1.8796 mL | 3.7592 mL | 7.5184 mL | 9.398 mL |
| 10 mM | 0.188 mL | 0.9398 mL | 1.8796 mL | 3.7592 mL | 4.699 mL |
| 50 mM | 0.0376 mL | 0.188 mL | 0.3759 mL | 0.7518 mL | 0.9398 mL |
| 100 mM | 0.0188 mL | 0.094 mL | 0.188 mL | 0.3759 mL | 0.4699 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively. Phase 2.
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Olopatadine hydrochloride and rupatadine fumarate in seasonal allergic rhinitis: A comparative study of efficacy and safety.[Pubmed:22025856]
J Pharmacol Pharmacother. 2011 Oct;2(4):270-6.
OBJECTIVE: To compare the efficacy and safety of olopatadine and rupatadine in seasonal allergic rhinitis (SAR). MATERIALS AND METHODS: A 2-week, single-centered, randomized, open, parallel group comparative clinical study was conducted on patients with SAR. Following inclusion and exclusion criteria, 70 patients were recruited and were randomized to two treatment groups and received the respective drugs for 2 weeks. At follow-up, clinical improvement was assessed in terms of change in total and differential count of leucocytes, serum Immunoglobulin E (IgE) level, Total Nasal Symptom Score (TNSS) and Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ) scoring. RESULTS: Both the drugs significantly reduced the differential count (P<0.001) and absolute eosinophil count (P<0.001), but olopatadine was found to be superior. In olopatadine group, there was significantly higher reduction in serum IgE (P=0.01), TNSS (P<0.001) and RQLQ score (P=0.015) than that of rupatadine. Incidence of adverse effects was found to be less in olopatadine group when compared with rupatadine group. CONCLUSIONS: Olopatadine is a better choice in SAR in comparison to rupatadine due to its better efficacy and safety profile.
Fixed drug eruption against rupatadine fumarate.[Pubmed:21959412]
J Craniofac Surg. 2011 Sep;22(5):1682-3.
Second generation of antihistaminics have better therapeutic efficacy and more predictable pharmacological responses at lower doses than older compounds. However, new compounds have a reduced adverse reaction profile; clinicians can also encounter some unexpected adverse effects of these newer compounds. We report the first case of fixed drug eruption of Rupatadine Fumarate, which was confirmed by oral provocation test.
Futura study: evaluation of efficacy and safety of rupatadine fumarate in the treatment of persistent allergic rhinitis.[Pubmed:19893935]
Braz J Otorhinolaryngol. 2009 Sep-Oct;75(5):673-9.
UNLABELLED: Allergic rhinitis affects 10-30% of the population, negatively impacting one's quality of life and productivity. It has been associated with sinusitis, otitis media, sleep disorders, and asthma. Rupatadine is a second generation antihistamine with increased affinity to histamine receptor H1; it is also a potent PAF (platelet-activating factor) antagonist. It starts acting quite quickly, offers long lasting effect, and reduces the chronic effects of rhinitis. AIM: this study aims to assess the efficacy and safety of rupatadine in the treatment of persistent allergic rhinitis. MATERIALS AND METHOD: this is a multi-centric open prospective study. This study included 241 patients from 13 centers in Brazil and was held between October of 2004 and August of 2005. Signs and symptoms of rhinitis and tolerance to medication were analyzed after one and two weeks of treatment. RESULTS: reduction on general scores from 8.65 to 3.21 on week 2 (p<0.001). All signs and symptoms improved significantly in the first day of treatment (p<0.001), except for nasal congestion and secretion, which improved from the second day of treatment (p<0.001). Adverse events occurred in 19.9% of the cases, 27.7% on week 1. CONCLUSION: rupatadine effectively controls persistent allergic rhinitis; it is safe and presents low incidence of side effects.
