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| Other Sizes |
| Targets |
Thiamine transporter (thiamine uptake mechanism in Eimeria species). Amprolium HCl acts as a thiamine antagonist by structurally mimicking thiamine (vitamin B1) and competitively blocking the thiamine transporter of Eimeria parasites. This inhibition prevents thiamine uptake, leading to impaired carbohydrate synthesis and energy metabolism in the parasite, ultimately resulting in its death. The compound does not act through conventional receptor targets but rather through direct competition for thiamine transport mechanisms.
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| ln Vitro |
Amprolium HCl demonstrates potent anticoccidial activity in vitro by inhibiting the growth and replication of Eimeria species in cell culture systems. The compound prevents carbohydrate synthesis in the parasite by blocking thiamine uptake, thereby disrupting essential metabolic pathways. Its efficacy has been characterized in various in vitro assays using Eimeria-infected cell cultures, with activity correlated to thiamine antagonism. The compound shows selective toxicity toward parasites due to their dependence on exogenous thiamine uptake.
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| ln Vivo |
In vivo, Amprolium HCl is effective as a prophylactic and therapeutic anticoccidial agent in poultry. It is administered via drinking water or feed to prevent and treat coccidiosis caused by Eimeria species. The compound reduces oocyst shedding, intestinal lesions, and mortality associated with coccidial infection. Its efficacy has been demonstrated in numerous field and controlled studies in commercial poultry operations. The compound is well-tolerated at therapeutic doses in chickens and turkeys.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Amprolium HCl are not typically performed, as the compound acts through thiamine transport inhibition rather than enzyme or receptor binding. Thiamine uptake inhibition assays can be conducted using Eimeria cell cultures or isolated parasites. Parasites are incubated with radiolabeled thiamine in the presence of varying concentrations of Amprolium HCl, and thiamine uptake is measured. IC50 values for thiamine transport inhibition can be determined from dose-response curves.
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| Cell Assay |
Cellular assays for Amprolium HCl involve culturing Eimeria species in suitable host cell lines. Infected cells are treated with Amprolium HCl at varying concentrations (typically 0.1-100 µg/mL) for 24-72 hours. Parasite growth and replication are assessed by microscopic examination, oocyst counting, or molecular methods such as qPCR. Cytotoxicity toward host cells is assessed using standard viability assays such as MTT. The selectivity index is calculated by comparing parasite inhibition to host cell toxicity.
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| Animal Protocol |
In vivo animal studies for Amprolium HCl are conducted in poultry models of coccidiosis. Chickens or turkeys are infected with Eimeria oocysts and treated with Amprolium HCl via drinking water or feed at doses ranging from 125-250 ppm. Efficacy endpoints include oocyst shedding, intestinal lesion scores, weight gain, and mortality. The compound is typically administered for 5-7 days, and protection is assessed by comparison to infected untreated controls.
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| ADME/Pharmacokinetics |
Amprolium HCl is administered orally via drinking water or feed. The compound is soluble in DMSO at 2 mg/mL (6.34 mM). It is excreted primarily via the renal route. Withdrawal periods are established for poultry products to ensure food safety. The compound has a molecular weight of 315.24 and a molecular formula of C14H20Cl2N4. It should be stored as a powder at -20°C for up to 3 years.
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| Toxicity/Toxicokinetics |
Amprolium HCl is generally well-tolerated in poultry at therapeutic doses. Overdose may lead to thiamine deficiency symptoms including anorexia, weight loss, and neurological signs. The compound is not approved for human therapeutic use. Standard safety precautions should be taken when handling the compound, including the use of personal protective equipment. Withdrawal periods must be observed to prevent residues in meat and eggs.
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| Additional Infomation |
Amprolium is an anticoccidial drug used in poultry. It is a veterinary anticoccidial drug that interferes with thiamine metabolism. See also: Amprolium ion (containing the active moiety); Amprolium; Ethoxybenzoate (ingredient); Amprolium; Banbemycin (ingredient)... See more...
Amprolium HCl is a thiamine antagonist anticoccidial drug used exclusively in veterinary medicine, particularly in poultry production. It is not approved for human use and is available only for veterinary and research purposes. The compound is also known by synonyms including Amprolium chloride and Amprovine. Its mechanism of action involves competitive inhibition of thiamine transport in Eimeria parasites. The compound is typically formulated as a soluble powder or liquid concentrate for administration via drinking water. |
| Molecular Formula |
C14H20CL2N4
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|---|---|
| Molecular Weight |
315.242
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| Exact Mass |
314.106
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| CAS # |
137-88-2
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| Related CAS # |
Amprolium;121-25-5
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| PubChem CID |
8732
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| Appearance |
White to off-white solid powder
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| Melting Point |
241 °C
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| LogP |
0.042
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
246
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].[Cl-].[N+]1(=C([H])C([H])=C([H])C([H])=C1C([H])([H])[H])C([H])([H])C1=C([H])N=C(C([H])([H])C([H])([H])C([H])([H])[H])N=C1N([H])[H]
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| InChi Key |
PJBQYZZKGNOKNJ-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C14H19N4.2ClH/c1-3-6-13-16-9-12(14(15)17-13)10-18-8-5-4-7-11(18)2/h4-5,7-9H,3,6,10H2,1-2H3,(H2,15,16,17)2*1H/q+1/p-1
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| Chemical Name |
1-((4-amino-2-propylpyrimidin-5-yl)methyl)-2-methylpyridin-1-ium chloride hydrochloride
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| Synonyms |
Amprol Amprol 25 Thiacoccid NSC523454 NSC-523454NSC 523454 Amprolium HCl
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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) |
H2O : ≥ 200 mg/mL (~634.44 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (317.22 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1722 mL | 15.8609 mL | 31.7219 mL | |
| 5 mM | 0.6344 mL | 3.1722 mL | 6.3444 mL | |
| 10 mM | 0.3172 mL | 1.5861 mL | 3.1722 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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