| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Cytochrome bc1 complex (also known as complex III of the mitochondrial electron transport chain). The cytochrome bc1 complex is essential for mitochondrial respiration and ATP production in eukaryotic cells. Inhibition of the cytochrome bc1 complex disrupts the electron transport chain, leading to reduced ATP synthesis and parasite death. DNDI-6174 targets this complex in Leishmania parasites.
|
|---|---|
| ln Vitro |
DNDI-6174 has potent in vitro activity against a variety of Leishmania species. It works by disrupting parasite-specific metabolic pathways. Detailed in vitro activity data (EC50, IC50) are not provided in the available literature. As a cytochrome bc1 inhibitor, it reduces parasite viability and proliferation in culture.
|
| ln Vivo |
DNDI-6174 can reduce parasite burden in animal models of infection. It is a preclinical candidate for visceral leishmaniasis, showing promise in preclinical models for efficacy and safety. In vivo studies have demonstrated reduction of parasite burden in infected animals. Further details on specific animal models and dosing regimens are not available.
|
| Enzyme Assay |
In vitro enzyme inhibition assays are performed using purified cytochrome bc1 complex or mitochondrial preparations incubated with varying concentrations of DNDI-6174. Enzyme activity is measured by monitoring cytochrome c reduction or oxygen consumption. IC50 values are determined from dose-response curves. DNDI-6174 shows potent inhibition of the Leishmania cytochrome bc1 complex.
|
| Cell Assay |
Leishmania parasites (various species) are cultured in vitro and treated with DNDI-6174 at varying concentrations. Parasite viability and proliferation are assessed using standard assays (e.g., resazurin reduction, Alamar Blue). IC50 values are calculated from dose-response curves. DNDI-6174 demonstrates potent activity against multiple Leishmania species.
|
| Animal Protocol |
Animal models of visceral leishmaniasis (e.g., Leishmania donovani-infected mice or hamsters) are administered DNDI-6174 via oral or intraperitoneal routes. Parasite burden in liver and spleen is assessed by limiting dilution culture or qPCR. DNDI-6174 reduces parasite burden in infected animals.
|
| ADME/Pharmacokinetics |
DNDI-6174 is a nitroimidazole-based drug candidate with favorable pharmacokinetic properties. It is orally bioavailable and reaches therapeutic concentrations in tissues affected by Leishmania infection. Detailed PK parameters (Cmax, Tmax, AUC, t1/2) have been evaluated in preclinical studies but are not publicly available in the search results.
|
| Toxicity/Toxicokinetics |
DNDI-6174 is a preclinical candidate with a favorable safety profile in preclinical models. As a cytochrome bc1 inhibitor, potential toxicities may include effects on host mitochondrial function, although selective targeting of parasite cytochrome bc1 may reduce host toxicity. Standard toxicology studies are required for therapeutic development.
|
| References | |
| Additional Infomation |
DNDI-6174 is a research-grade cytochrome bc1 complex inhibitor for antiparasitic research. CAS: 2868298-43-3. Molecular formula: C16H13N5O2, molecular weight: 307.31. It is a preclinical candidate for visceral leishmaniasis with potent in vitro activity against Leishmania species and reduces parasite burden in animal models. For research use only.
|
| CAS # |
2868298-43-3
|
|---|---|
| Appearance |
White to off-white solid powder
|
| 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 |
| 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) |
DMSO :~100 mg/mL (~325.40 mM; with sonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.14 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 and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up 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: ≥ 2.5 mg/mL (8.14 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 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD saline solution and mix well. 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: ≥ 2.5 mg/mL (8.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution. |
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
