Pyronaridine TetraphosphateAntimalarial agent CAS# 76748-86-2 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 76748-86-2 | SDF | Download SDF |
| PubChem ID | 5488630 | Appearance | Powder |
| Formula | C29H32ClN5O24H3PO4 | M.Wt | 968.0 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 25 mg/mL (27.47 mM; Need ultrasonic and warming) | ||
| Chemical Name | 4-[(7-chloro-2-methoxy-1,5-dihydrobenzo[b][1,5]naphthyridin-10-yl)imino]-2,6-bis(pyrrolidin-1-ylmethyl)cyclohexa-2,5-dien-1-one;phosphoric acid | ||
| SMILES | COC1=CC=C2C(=C(C3=C(N2)C=C(C=C3)Cl)N=C4C=C(C(=O)C(=C4)CN5CCCC5)CN6CCCC6)N1.OP(=O)(O)O.OP(=O)(O)O.OP(=O)(O)O.OP(=O)(O)O | ||
| Standard InChIKey | JDVZOLDKAQEQDD-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C29H32ClN5O2.4H3O4P/c1-37-26-9-8-24-28(33-26)27(23-7-6-21(30)16-25(23)32-24)31-22-14-19(17-34-10-2-3-11-34)29(36)20(15-22)18-35-12-4-5-13-35;4*1-5(2,3)4/h6-9,14-16,32-33H,2-5,10-13,17-18H2,1H3;4*(H3,1,2,3,4) | ||
| 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 | Pyronaridine Tetraphosphate is a common antimalarial agent. | |||||
| Targets | MDR multidrug resistance | |||||
Pyronaridine Tetraphosphate Dilution Calculator
Pyronaridine Tetraphosphate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.0331 mL | 5.1653 mL | 10.3306 mL | 20.6612 mL | 25.8264 mL |
| 5 mM | 0.2066 mL | 1.0331 mL | 2.0661 mL | 4.1322 mL | 5.1653 mL |
| 10 mM | 0.1033 mL | 0.5165 mL | 1.0331 mL | 2.0661 mL | 2.5826 mL |
| 50 mM | 0.0207 mL | 0.1033 mL | 0.2066 mL | 0.4132 mL | 0.5165 mL |
| 100 mM | 0.0103 mL | 0.0517 mL | 0.1033 mL | 0.2066 mL | 0.2583 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. | |||||
Abstract
PNDP, an antimalarial drug, could barely cross the blood-brain barrier and exhibited gender-independent pharmacokinetics where orally administered PNDP was readily absorbed from the small intestine, widely distributed in tissues and excreted in urine, feces and breath with similar values of C(max), AUC(0-inf) and T(max) to those in previous studies.
Abstract
Pyronaridine tetraphosphate is a water-soluble tetraphosphate salt of pyronaridine, an antimalarial drug, and has significant light absorption in the range of 190-380 nm.
Abstract
Plasma and blood specimens from a rabbit pretreated with pyronnaridine tetraphosphate were analyzed by a high-performance liquid chromatography method.
Abstract
Blood and urine samples from a monkey pretreated with pyronaridine tetraphosphate were analyzed by a high-performance liquid chromatographic method.
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Pyronaridine (PND), a synthetic quinolone derivative frequently prescribed for the treatment of malaria, is a selective and potent multidrug resistance (MDR) modulator of Pgp-mediated MDR that inhibits the proliferation of a variety of tumor cells, including myeloid leukemia (K562 and K562/A02), epidermoid carcinoma (KB and KBV200), breast carcinoma (MCF-7 and MCF-7/ADR), ovarian carcinoma (SKOV3, ES-2 and PA-1), gastric carcinoma (BGC-823), colon carcinoma (LoVo), hepatocellular carcinoma (SMMZ-7721 and QGY-7703), with the half maximal inhibition concentration IC50 values of 8.3 μM, 5.6 μM, 20.8 μM, 14.5 μM, 9.5 μM, 11 μM, 9.7 μM, 12.9 μM, 15.7 μM, 14.9 μM, 21.4 μM, 10.9 μM and 17.1 μM respectively [1].
References:
[1] Qi J, Wang S, Liu G, Peng H, Wang J, Zhu Z, Yang C. Pyronaridine, a novel modulator of P-glycoprotein-mediated multidrug resistance in tumor cells in vitro and in vivo. Biochem Biophys Res Commun. 2004 Jul 9;319(4):1124-31.
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Absorption, distribution, excretion, and pharmacokinetics of 14C-pyronaridine tetraphosphate in male and female Sprague-Dawley rats.[Pubmed:20379367]
J Biomed Biotechnol. 2010;2010:590707.
The main objective of this investigation was to determine the absorption, distribution, excretion, and pharmacokinetics of the antimalarial drug Pyronaridine Tetraphosphate (PNDP) in Sprague-Dawley rats. Following oral administration of a single dose (10 mg/Kg) of 14C-PNDP, it was observed that the drug was readily absorbed from the small intestine within 1 hour following oral administration and was widely distributed in most of the tissues investigated as determined from the observed radioactivity in the tissues. The peak value of the drug in the blood was reached at around 8 hours postadministration, and radioactivity was detected in most of the tissues from 4 hours onwards. 14C-PNDP showed a poor permeability across the blood-brain barrier, and the absorption, distribution, and excretion of 14C-PNDP were found to be gender-independent as both male and female rats showed a similar pattern of radioactivity. Excretion of the drug was predominantly through the urine with a peak excretion post 24 hours of administration. A small amount of the drug was also excreted in the feces and also in the breath. It was found that the C(max), AUC (0-inf), and T(max) values were similar to those observed in the Phase II clinical trials of pyronaridine/artesunate (Pyramax) conducted in Uganda.
