| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g | |||
| 2g | |||
| 5g | |||
| Other Sizes |
| Targets |
The primary target of Pyrantel tartrate is the nicotinic acetylcholine receptor (nAChR) on the body wall muscle of susceptible nematodes. It acts as an agonist of these receptors. By binding to and persistently activating these excitatory nAChRs, Pyrantel tartrate causes a prolonged depolarization of the muscle cell membrane. This depolarizing action results in spastic muscle paralysis in the parasites. The paralyzed worms are then unable to maintain their position in the host's intestinal tract and are eventually expelled through the feces.
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| ln Vitro |
For 72 hours, pyrantel tartrate (10 nM–10 µM) demonstrated strong anti-A antibodies. suum and anti-N (0-168.2 M; 72 h). Activities of American Nus [1][2].
In vitro, Pyrantel tartrate demonstrates potent anthelmintic activity by acting as an agonist of the nicotinic acetylcholine receptor (nAChR). Its mechanism involves causing spasmodic muscle paralysis in parasitic worms due to prolonged activation of the excitatory nACh receptors on the body wall muscle. At the molecular level, it is known to promote the release of acetylcholine and inhibit cholinesterase, further contributing to the sustained depolarization of the neuromuscular junction. This leads to a spastic paralysis that is the hallmark of its anthelmintic effect in vitro. |
| ln Vivo |
In hamsters infected with Vibrio ceylonali, pyrantel tartrate (10 mg/kg; po; single dose) can reduce the number of worms, reducing the worm burden by 87.2% and deworming rate to 63.4% [2].
In vivo, Pyrantel tartrate is administered orally as an anthelmintic. Following oral administration, it acts locally in the gastrointestinal tract to paralyze parasitic worms. The paralyzed worms are then expelled from the body through normal peristalsis. A single dose is often effective for many common worm infections. It is used in both human and veterinary medicine, with the tartrate salt being a common form for research and veterinary applications. Its efficacy is well-established, and it is considered a safe and effective treatment for a range of nematode infections. |
| Enzyme Assay |
Cell-free receptor binding assays for Pyrantel tartrate typically use membrane preparations from nematode muscle tissue or from cells expressing recombinant nematode nicotinic acetylcholine receptors. A standard protocol involves incubating the receptor-containing membranes with a radiolabeled ligand, such as [3H]-epibatidine or [125I]-alpha-bungarotoxin, and varying concentrations of Pyrantel tartrate. The bound and free ligand are separated by filtration, and the radioactivity is measured. The binding affinity (IC50 or Ki) is determined by competitive displacement curves, which helps characterize the compound's interaction with the nAChR.
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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 in vitro cellular experiments, cell lines expressing nematode nicotinic acetylcholine receptors are used. Cells are seeded in multi-well plates and treated with Pyrantel tartrate at various concentrations (typically 0.1-100 uM). Receptor activation is assessed using calcium flux assays, where the influx of calcium ions upon receptor activation is measured using a fluorescent calcium indicator (e.g., Fluo-4). Alternatively, electrophysiological techniques such as patch-clamp can be employed to directly measure the ionic currents induced by Pyrantel tartrate, providing precise data on its agonistic activity. |
| 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 animal experiments with Pyrantel tartrate are typically conducted in animal models of parasitic infection, such as mice or hamsters infected with nematodes like Heligmosomoides polygyrus or Trichinella spiralis. A common protocol involves infecting the animals with the parasite, followed by oral administration of Pyrantel tartrate at various doses (e.g., 1-50 mg/kg). The compound's efficacy is assessed by counting the number of worms remaining in the gastrointestinal tract after euthanasia. The reduction in worm burden compared to an untreated control group indicates the compound's anthelmintic activity. |
| ADME/Pharmacokinetics |
Pyrantel tartrate has a molecular weight of 356.39 g/mol and a chemical formula of C15H20N2O6S. It is a salt that is administered orally. As an anthelmintic that acts locally in the gastrointestinal tract, it is poorly absorbed systemically, which contributes to its favorable safety profile. Its half-life is short, and it is primarily excreted in the feces. It is formulated for oral administration as a suspension or in tablet form for both human and veterinary use. It should be stored at room temperature, protected from light and moisture.
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| Toxicity/Toxicokinetics |
Pyrantel tartrate has a well-established safety and toxicity profile. It is generally well-tolerated, with common side effects being mild and transient, including gastrointestinal disturbances such as nausea, vomiting, and diarrhea. As a depolarizing neuromuscular blocker, it is specific for parasitic nAChRs, which limits its toxicity in mammalian hosts. However, high doses can cause more severe neurological effects. It is contraindicated in patients with liver dysfunction and should be used with caution in patients with a history of epilepsy. It is for research use only and not for human therapeutic use in a research setting.
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| References |
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| Additional Infomation |
Broad-spectrum anthelmintic for livestock. See also: Praziquantel (contains active ingredient); Carbadox; Praziquantel tartrate (ingredient); Praziquantel tartrate; Tylosin phosphate (ingredient)... See more...
Pyrantel tartrate is a pyrimidine-derivative anthelmintic agent used for the oral treatment of various parasitic worm infections. Its mechanism involves acting as an agonist of the nicotinic acetylcholine receptor (nAChR), leading to spastic muscle paralysis in parasites. It was first described in 1965 and is on the WHO List of Essential Medicines. In humans, it is typically administered as the pamoate salt. It is a safe and effective drug, often requiring only a single dose for effective treatment, and is widely used in both human and veterinary medicine. |
| Molecular Formula |
C11H14N2S.C4H6O6
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|---|---|
| Molecular Weight |
356.3941
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| Exact Mass |
356.104
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| CAS # |
33401-94-4
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| Related CAS # |
Pyrantel pamoate;22204-24-6;Pyrantel;15686-83-6
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| PubChem CID |
6434144
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
324.4ºC at 760 mmHg
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| Melting Point |
148-150ºC
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| Flash Point |
150ºC
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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 |
5
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| Heavy Atom Count |
24
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| Complexity |
382
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CN1CCCN=C1/C=C/C2=CC=CS2.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
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| InChi Key |
VWRCYAZJKNPEQR-NIEARKAZSA-N
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| InChi Code |
InChI=1S/C11H14N2S.C4H6O6/c1-13-8-3-7-12-11(13)6-5-10-4-2-9-14-10;5-1(3(7)8)2(6)4(9)10/h2,4-6,9H,3,7-8H2,1H3;1-2,5-6H,(H,7,8)(H,9,10)/b6-5+;/t;1-,2-/m.1/s1
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| Chemical Name |
(2R,3R)-2,3-dihydroxybutanedioic 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 : ≥ 34 mg/mL (~95.40 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8059 mL | 14.0296 mL | 28.0591 mL | |
| 5 mM | 0.5612 mL | 2.8059 mL | 5.6118 mL | |
| 10 mM | 0.2806 mL | 1.4030 mL | 2.8059 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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