| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Toxoplasma gondii[1]
The primary target of arprinocid is parasites, including coccidia and Toxoplasma gondii. The compound works by disrupting the energy metabolism of these parasites, leading to their death. Arprinocid and its main metabolite, arprinocid-1-N-oxide, have been found to exert a cidal effect on Toxoplasma gondii in vitro. The compound is a member of 6-aminopurines. |
|---|---|
| ln Vitro |
In vitro studies have demonstrated that arprinocid is active against Toxoplasma gondii. The compound and its main metabolite, arprinocid-1-N-oxide, exert a cidal effect on T. gondii in vitro. Arprinocid is a purine analog with activity against murine T. gondii. These in vitro activities support its use as an antiparasitic agent.
|
| ln Vivo |
Arprinocid exhibited potent in vivo activity against murine toxoplasmosis.
In vivo studies have confirmed the antiparasitic activity of arprinocid. The compound is an anticoccidial agent used in poultry. It has been developed to combat coccidia in animals. Arprinocid's in vivo efficacy has been demonstrated in animal models. |
| Enzyme Assay |
For antiparasitic activity screening, standard in vitro assays using parasites are used. Parasites are cultured in appropriate media and exposed to serial dilutions of arprinocid. Parasite viability is assessed, and IC₅₀ values are calculated.
|
| Cell Assay |
For in vitro cell-based studies, T. gondii or other parasites are cultured in appropriate media and treated with serial dilutions of arprinocid. Parasite viability is assessed using standard assays. Cytotoxicity against host cells is assessed in parallel.
|
| Animal Protocol |
In vivo animal studies for arprinocid have been conducted in poultry and other animal models. The compound is administered via feed or other routes. Efficacy endpoints include reduction in parasite burden and improvement in clinical parameters.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of arprinocid have been characterized. The compound has a melting point of 245-246°C. Specific PK parameters such as half-life and bioavailability have been reported in the literature. The main metabolite is arprinocid-1-N-oxide.
|
| Toxicity/Toxicokinetics |
Toxicological data for arprinocid are available from regulatory submissions for veterinary use. The compound has been evaluated for safety in animals. Standard toxicology studies have been conducted for veterinary approval.
|
| References |
[1]. Luft BJ. Potent in vivo activity of arprinocid, a purine analogue, against murine toxoplasmosis. J Infect Dis. 1986 Oct;154(4):692-4.
|
| Additional Infomation |
Arprinocid belongs to the 6-aminopurine class of drugs.
Antibacterium A drug that kills parasites. Used to treat helminthiasis in humans and animals. Anticoccidial drugs A drug used to treat or prevent coccidiosis in humans and animals. Arprinocid is an anticoccidial agent used in veterinary medicine. It is a synthetic purine analog developed to combat parasites in poultry. The compound is also active against Toxoplasma gondii. Arprinocid is available as a research compound for antiparasitic studies. No human clinical trials have been reported. |
| Molecular Formula |
C12H9CLFN5
|
|---|---|
| Molecular Weight |
277.68
|
| Exact Mass |
277.053
|
| Elemental Analysis |
C, 51.90; H, 3.27; Cl, 12.77; F, 6.84; N, 25.22
|
| CAS # |
55779-18-5
|
| PubChem CID |
41574
|
| Appearance |
White to off-white powder
|
| Density |
1.6±0.1 g/cm3
|
| Boiling Point |
504.6±60.0 °C at 760 mmHg
|
| Melting Point |
441ºC
|
| Flash Point |
259.0±32.9 °C
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
| Index of Refraction |
1.732
|
| LogP |
1.73
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
19
|
| Complexity |
321
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
NC1=C2N=CN(CC3=C(F)C=CC=C3Cl)C2=NC=N1
|
| InChi Key |
NAPNOSFRRMHNBJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H9ClFN5/c13-8-2-1-3-9(14)7(8)4-19-6-18-10-11(15)16-5-17-12(10)19/h1-3,5-6H,4H2,(H2,15,16,17)
|
| Chemical Name |
9-[(2-chloro-6-fluorophenyl)methyl]purin-6-amine
|
| Synonyms |
Arprinocid; 55779-18-5; 9-(2-Chloro-6-fluorobenzyl)-9H-purin-6-amine; Arpocox; Arprinocide; 9-[(2-chloro-6-fluorophenyl)methyl]purin-6-amine; 9-(2-Chloro-6-fluorobenzyl)adenine; 9-[(2-Chloro-6-fluorophenyl)methyl]-9H-purin-6-amine;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6013 mL | 18.0063 mL | 36.0127 mL | |
| 5 mM | 0.7203 mL | 3.6013 mL | 7.2025 mL | |
| 10 mM | 0.3601 mL | 1.8006 mL | 3.6013 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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