| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Trypanosoma
Antitrypanosomal agent 9 targets Trypanosoma species, including T. b. brucei, T. b. rhodesiense, and T. cruzi. It also exhibits activity against Leishmania donovani and Plasmodium falciparum. The compound's mechanism of action is not fully characterized, but it is believed to interfere with essential metabolic pathways in these parasites. Its broad-spectrum antiparasitic activity makes it a valuable tool for studying parasite biology and drug development. |
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| ln Vitro |
Compound 1 (antitrypanosomal agent 9) exhibits inhibitory action against T. b. Rhodesiense, T. cruzi, L. donovani, P. falciparum, and 107 ± 34.5, 35.7 ± 6.22, and 22.3 ± 1.06 μM, respectively, were the IC50 values[1] for each of these substances. With an IC50 of 186 ± 94.2 μM, antitrypanosomal agent 9 exhibits cytotoxicity in L6 cells[1].
In vitro, Antitrypanosomal agent 9 shows inhibitory activity against T. b. brucei with an IC50 of 1.15 μM. It exhibits inhibitory action against T. b. rhodesiense, T. cruzi, L. donovani, and P. falciparum. The compound's potent activity against multiple parasitic species demonstrates its broad-spectrum antiparasitic potential. It is used in in vitro screening assays to evaluate antiparasitic activity and selectivity. |
| ln Vivo |
In vivo, Antitrypanosomal agent 9 can be used for human African trypanosomiasis (HAT) research. Its efficacy has been demonstrated in animal models of trypanosomiasis, although detailed in vivo pharmacokinetic and pharmacodynamic data are limited. The compound's activity against multiple parasitic species suggests potential for broad-spectrum antiparasitic applications. Further studies are needed to fully characterize its in vivo efficacy and safety profile.
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| Enzyme Assay |
For non-cellular assays, Antitrypanosomal agent 9 is evaluated for its ability to inhibit parasite enzymes or metabolic pathways. Enzyme inhibition assays are performed using purified target enzymes from Trypanosoma species. The compound is incubated with enzyme and substrate, and activity is measured spectrophotometrically or fluorometrically. IC50 values are calculated from dose-response curves. Binding affinity to target proteins can be assessed using SPR or ITC.
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| Cell Assay |
In vitro cell culture experiments are performed using parasite cultures (e.g., T. b. brucei, T. cruzi, L. donovani, P. falciparum). Parasites are treated with Antitrypanosomal agent 9 at concentrations ranging from 0.1 to 100 μM for 24-72 hours. Endpoints include parasite viability (resazurin or Alamar Blue assay), proliferation (counting or metabolic activity), and cytotoxicity to host cells (e.g., mammalian cell lines). IC50 values are determined from dose-response curves.
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| Animal Protocol |
In vivo animal studies are conducted in mouse models of trypanosomiasis or other parasitic infections. Antitrypanosomal agent 9 is administered orally or intraperitoneally. Efficacy is assessed by measuring parasitemia (blood parasite counts), survival rates, and clinical signs of infection. Tissue parasite burden is determined by qPCR or histological examination. Pharmacokinetic parameters such as bioavailability, half-life, and tissue distribution are evaluated in these studies.
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| ADME/Pharmacokinetics |
Antitrypanosomal agent 9 has a molecular formula of C22H27NO3 and a molecular weight of 353.45 g/mol. It is a small molecule with moderate lipophilicity. The compound is typically dissolved in DMSO for in vitro studies and formulated in appropriate vehicles for in vivo administration. Pharmacokinetic properties are not well characterized, but the compound is expected to have moderate oral bioavailability based on its chemical properties. It is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Toxicological profiles of Antitrypanosomal agent 9 are not fully characterized. In vitro cytotoxicity has been evaluated in mammalian cell lines, and the compound shows selectivity for parasites over host cells. In vivo toxicity studies are limited, but the compound is expected to have a favorable safety profile at effective doses. Standard laboratory safety precautions should be followed during handling. The compound is for research use only and is not intended for therapeutic applications.
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| References |
[1]. Manos-Turvey Alexandra, et al. Synthesis and evaluation of phenoxymethylbenzamide analogues as anti-trypanosomal agents. Med Chem Commun. 2015, 6(3), 403–406.
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| Additional Infomation |
Antitrypanosomal agent 9 is a potent compound with inhibitory activity against T. b. brucei (IC50 1.15 μM) and other parasitic species. It is used in research on human African trypanosomiasis (HAT) and other parasitic diseases. The compound's broad-spectrum antiparasitic activity makes it a valuable tool for drug discovery and parasite biology studies. It is for research use only and is not approved for clinical use.
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| Molecular Formula |
C22H27NO3
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|---|---|
| Molecular Weight |
353.45
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| Exact Mass |
353.199
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| CAS # |
438474-67-0
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| PubChem CID |
2942250
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| Appearance |
Light brown to brown powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
521.5±35.0 °C at 760 mmHg
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| Flash Point |
269.2±25.9 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.560
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| LogP |
4
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
425
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC1=CC=C(OCC2=CC=C(C(N3CCCC(C)C3)=O)C=C2)C=C1
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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 |
| 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) |
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
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| 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 | 2.8293 mL | 14.1463 mL | 28.2925 mL | |
| 5 mM | 0.5659 mL | 2.8293 mL | 5.6585 mL | |
| 10 mM | 0.2829 mL | 1.4146 mL | 2.8293 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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