| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 25g |
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| Targets |
Pyrantel pamoate's primary target is the nicotinic acetylcholine receptor (nAChR) in nematodes. It acts as an agonist, activating these receptors and causing depolarizing neuromuscular blockade. This leads to spastic paralysis and expulsion of the worms.
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| ln Vitro |
The anti-A antibodies displayed by Pyrantel Pamoate (10 nM-10 µM; 72 hours) were good. suum and anti-N (0-168.2 M; 72 h). Activities of American Nus [1][2].
In vitro, Pyrantel pamoate is an agonist of nematode nAChRs. It activates chimeric C. elegans α7-nAChRs expressed in BOSC cells with an EC50 of 40 μM. It induces contraction of A. suum muscle with an EC50 of 57.5 nM. |
| ln Vivo |
Pyrantel pamoate (10 mg/kg; po; single dose) can reduce the number of worms in hamsters infected with Vibrio ceylonali, reducing the worm load by 87.2%, and the deworming rate reaches 63.4% [2].
In vivo, Pyrantel pamoate is used as an anthelmintic to treat nematode infections. It is effective against various parasitic worms, including Ascaris, hookworms, and pinworms. It is administered orally and acts locally in the gastrointestinal tract. |
| Enzyme Assay |
The in vitro activity of Pyrantel pamoate is assessed using electrophysiological techniques and muscle contraction assays. The compound's effect on nAChR-mediated currents in cells expressing the receptor or on muscle contraction in parasitic worms is measured.
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| Cell Assay |
Cell viability assay [2]
Cell Types: Nepenthes americana Tested Concentrations: 0-168.2 M (0-100 µg/mL) Incubation Duration: 72 hrs (hours) Experimental Results: Inhibitory effect on third-stage larvae and adults of Nepenthes americana, IC50 The values are 2.0 and 7.6 mg/ml respectively. For cellular assays, cells expressing nematode nAChRs are used. Cells are treated with various concentrations of Pyrantel pamoate, and the activation of the receptor is measured using electrophysiological or calcium imaging techniques. |
| Animal Protocol |
Animal/Disease Models: Male Syrian golden hamster (3 weeks old; A. ceylanicum infection) [2].
Doses: 10 mg/kg Route of Administration: Oral; single. Experimental Results: The worm load reduction rate and deworming rate were 87.2% and 63.4% respectively. In vivo, Pyrantel pamoate is administered orally to animals or humans. Its efficacy is assessed by measuring the reduction in egg counts or the clearance of worms from the gastrointestinal tract. |
| ADME/Pharmacokinetics |
Pyrantel pamoate has a molecular weight of 594.68 g/mol and a molecular formula of C11H14N2S·C23H16O6. It is a yellow to tan solid. It should be stored at 0-10°C under refrigeration, in an inert gas and protected from air and heat.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation There is currently no information regarding the use of Pyrantel during lactation. This drug is poorly absorbed orally and is therefore unlikely to be excreted into breast milk or absorbed by breastfed infants. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk As of the revision date, no relevant published information was found. Pyrantel pamoate is generally well-tolerated. Common side effects include gastrointestinal disturbances such as nausea, vomiting, abdominal pain, and diarrhea. It is contraindicated in patients with hepatic impairment. |
| References |
[1]. Martin RJ, et, al. Oxantel is an N-type (methyridine and nicotine) agonist not an L-type (levamisole and pyrantel) agonist: classification of cholinergic anthelmintics in Ascaris. Int J Parasitol. 2004 Aug;34(9):1083-90.
[2]. Tritten L, et, al. In vitro and in vivo efficacy of Monepantel (AAD 1566) against laboratory models of human intestinal nematode infections. PLoS Negl Trop Dis. 2011 Dec;5(12):e1457. |
| Additional Infomation |
Pyrantel is an odorless, pale yellow to brownish-red crystalline powder, tasteless. It is used to treat nematode infections in animals. Pyrantel is an organic molecular entity. It is a broad-spectrum anti-nematode anthelmintic, also used in veterinary medicine. See also: Pyrantel (contains active ingredient); Pyrantel; Pyrantel (ingredient); Moxiquidine; Pyrantel; Saloranal (ingredient)... See more...
Pyrantel pamoate is a widely used anthelmintic drug. It is available over-the-counter in many countries for the treatment of pinworm infections. It is also used in veterinary medicine. Its mechanism of action as a nAChR agonist is well-established. |
| Molecular Formula |
C34H30N2O6S
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|---|---|
| Molecular Weight |
594.6768
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| Exact Mass |
594.182
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| CAS # |
22204-24-6
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| Related CAS # |
Pyrantel tartrate;33401-94-4;Pyrantel;15686-83-6
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| PubChem CID |
5281033
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
642.7ºC at 760 mmHg
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| Melting Point |
266-267ºC
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| Flash Point |
356.5ºC
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| Vapour Pressure |
2.13E-17mmHg at 25°C
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| LogP |
6.26
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
43
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| Complexity |
816
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C([H])=C([H])C([H])=C1/C(/[H])=C(\[H])/C1=NC([H])([H])C([H])([H])C([H])([H])N1C([H])([H])[H].O([H])C1C(C(=O)O[H])=C([H])C2=C([H])C([H])=C([H])C([H])=C2C=1C([H])([H])C1=C(C(C(=O)O[H])=C([H])C2=C([H])C([H])=C([H])C([H])=C12)O[H]
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| InChi Key |
AQXXZDYPVDOQEE-MXDQRGINSA-N
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| InChi Code |
InChI=1S/C23H16O6.C11H14N2S/c24-20-16(14-7-3-1-5-12(14)9-18(20)22(26)27)11-17-15-8-4-2-6-13(15)10-19(21(17)25)23(28)29;1-13-8-3-7-12-11(13)6-5-10-4-2-9-14-10/h1-10,24-25H,11H2,(H,26,27)(H,28,29);2,4-6,9H,3,7-8H2,1H3/b;6-5+
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| Chemical Name |
4-[(3-carboxy-2-hydroxynaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylic acid;1-methyl-2-[(E)-2-thiophen-2-ylethenyl]-5,6-dihydro-4H-pyrimidine
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~20.83 mg/mL (~35.03 mM ()
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6816 mL | 8.4079 mL | 16.8158 mL | |
| 5 mM | 0.3363 mL | 1.6816 mL | 3.3632 mL | |
| 10 mM | 0.1682 mL | 0.8408 mL | 1.6816 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.
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