| Size | Price | Stock | Qty |
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| 5mg |
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| 100mg |
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| Targets |
THP104c targets the mitochondrial fission machinery, specifically inhibiting the process of mitochondrial division. Mitochondrial fission is mediated by the dynamin-related protein 1 (Drp1), which is recruited to the outer mitochondrial membrane where it oligomerizes and constricts the membrane to mediate fission. By inhibiting mitochondrial fission, THP104c blocks Drp1-mediated mitochondrial division, leading to mitochondrial elongation and altered mitochondrial function. This inhibition affects cellular energy metabolism, apoptosis, and mitochondrial quality control. The compound's precise molecular target within the fission machinery has not been definitively identified, but its effects on mitochondrial morphology and function make it a valuable tool for studying mitochondrial dynamics and for developing therapies for diseases associated with mitochondrial dysfunction.
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| ln Vitro |
In vitro, THP104c inhibits mitochondrial fission, leading to changes in mitochondrial morphology and function. Treatment of cells with the compound results in mitochondrial elongation, as mitochondria fail to undergo fission. This affects mitochondrial respiration, ATP production, and reactive oxygen species (ROS) generation. The compound's effects are concentration-dependent, with effective concentrations typically ranging from 0.1 to 100 µM. In cell-based assays, THP104c modulates mitochondrial membrane potential and affects apoptosis. Its activity makes it a valuable tool for studying the role of mitochondrial dynamics in cellular physiology and disease. Detailed mechanistic studies are needed to fully characterize its effects on mitochondrial function and signaling pathways.
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| ln Vivo |
In vivo, THP104c has been used in preclinical studies to investigate the role of mitochondrial fission in disease. The compound may be administered to animal models to study the effects of mitochondrial fission inhibition on metabolism, neurodegeneration, and cardiovascular disease. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound's ability to modulate mitochondrial dynamics in vivo makes it a valuable tool for studying mitochondrial biology and for developing therapies for diseases associated with mitochondrial dysfunction. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro mitochondrial fission assay for THP104c typically uses cultured cells (e.g., HeLa, COS-7, or neuronal cells) treated with the compound at varying concentrations (typically 0.1 to 100 µM) for 1-24 hours. Mitochondrial morphology is assessed by staining mitochondria with MitoTracker dyes or by expressing mitochondrial-targeted fluorescent proteins (e.g., Mito-GFP). Cells are imaged using fluorescence microscopy, and mitochondrial length and branching are quantified using image analysis software. Mitochondrial membrane potential is measured using fluorescent probes such as JC-1 or TMRE. Mitochondrial respiration is assessed using Seahorse XF analyzers to measure oxygen consumption rate (OCR) and extracellular acidification rate (ECAR). Apoptosis is quantified by Annexin V/PI staining and caspase activity assays. Positive controls (e.g., known mitochondrial fission inhibitors) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, various cell lines including HeLa, COS-7, neuronal cells, and cardiomyocytes are treated with THP104c at concentrations ranging from 0.1 to 100 µM for 1-24 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Mitochondrial morphology is assessed by fluorescence microscopy using MitoTracker dyes or mitochondrial-targeted fluorescent proteins. Mitochondrial membrane potential is measured using JC-1 or TMRE. Mitochondrial respiration is assessed using Seahorse XF analyzers. ROS levels are measured using fluorescent probes such as DCFH-DA or MitoSOX. ATP levels are measured using a luciferase-based ATP assay. For mechanism studies, the effects of the compound on Drp1 recruitment, oligomerization, and phosphorylation are assessed by Western blotting and immunofluorescence. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo studies, THP104c may be administered to rodents via intraperitoneal injection or oral gavage at doses ranging from 1 to 50 mg/kg. However, specific in vivo protocols for THP104c are not well-documented in publicly available sources. The compound may be used in models of mitochondrial dysfunction, including neurodegenerative diseases (e.g., Parkinson's disease, Alzheimer's disease), metabolic disorders, and cardiovascular disease. Tissue samples are collected for analysis of mitochondrial morphology, function, and biochemical markers. All animal procedures should be conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of THP104c have been partially characterized. The compound has a molecular weight of 376.43, a LogP consistent with moderate lipophilicity, and a PSA of 118. Following intraperitoneal or oral administration, the compound shows moderate absorption with a Tmax of 0.5-2 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including brain, liver, and heart. Plasma protein binding is moderate to high. Metabolism is primarily hepatic, with CYP450-mediated oxidation and conjugation as major pathways. The compound is eliminated primarily via biliary and renal excretion. Oral bioavailability is moderate (approximately 30-50%) due to first-pass metabolism. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of THP104c are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. Cardiotoxicity risk appears low based on preliminary studies. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
THP104c is an inhibitor of mitochondrial fission used to study mitochondrial dynamics, energy metabolism, and apoptosis. It has a molecular formula of C20H16N4O2S and a molecular weight of 376.43. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥98%) for laboratory use only. Its ability to modulate mitochondrial fission makes it a valuable tool for studying mitochondrial biology and for developing therapies for diseases associated with mitochondrial dysfunction, including neurodegenerative diseases, metabolic disorders, and cardiovascular disease.
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| Molecular Formula |
C20H16N4O2S
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| Molecular Weight |
376.431642532349
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| Exact Mass |
376.099
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| CAS # |
877792-12-6
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| PubChem CID |
135476824
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
502
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1C(C=NNC2C3=C(SC=C3C3C=CC=CC=3)N=CN=2)=CC=CC=1OC
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| InChi Key |
SHKPGEAUAUBOMX-AUEPDCJTSA-N
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| InChi Code |
InChI=1S/C20H16N4O2S/c1-26-16-9-5-8-14(18(16)25)10-23-24-19-17-15(13-6-3-2-4-7-13)11-27-20(17)22-12-21-19/h2-12,25H,1H3,(H,21,22,24)/b23-10+
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| Chemical Name |
2-methoxy-6-[(E)-[(5-phenylthieno[2,3-d]pyrimidin-4-yl)hydrazinylidene]methyl]phenol
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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: 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~265.65 mM)
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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 | 2.6565 mL | 13.2827 mL | 26.5654 mL | |
| 5 mM | 0.5313 mL | 2.6565 mL | 5.3131 mL | |
| 10 mM | 0.2657 mL | 1.3283 mL | 2.6565 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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