| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Mitochondria, specifically the mitochondrial inner membrane. The triphenylphosphonium (TPP) cation is a delocalized lipophilic cation that accumulates several hundred-fold within mitochondria driven by the mitochondrial membrane potential (deltaΨm). By conjugating cholesterol to TPP, (R)-Chol-TPP can be targeted to mitochondria to study cholesterol trafficking, mitochondrial membrane dynamics, and cholesterol-related mitochondrial dysfunction.
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| ln Vitro |
In vitro, TPP-conjugated compounds accumulate in mitochondria in a membrane potential-dependent manner. The compound (R)-Chol-TPP is expected to be taken up by cells and localize to mitochondria, where it can modulate mitochondrial cholesterol content. Mitochondrial cholesterol accumulation is associated with various diseases including metabolic syndrome, neurodegenerative diseases, and certain cancers. The (R)-enantiomer designation indicates specific stereochemistry at the chiral center, which may affect biological activity.
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| ln Vivo |
In vivo activity of TPP-conjugated compounds is typically evaluated in rodent models of mitochondrial dysfunction. TPP-targeted compounds are orally or intravenously administered and accumulate in mitochondria of various tissues, particularly in organs with high mitochondrial density such as liver, heart, kidney, and brain. (R)-Chol-TPP may be used to study the role of mitochondrial cholesterol in disease processes. No therapeutic in vivo activity data is publicly available for this specific compound.
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| Enzyme Assay |
For mitochondrial accumulation studies, isolated mitochondria from rat liver or heart are prepared by differential centrifugation. Mitochondria are resuspended in assay buffer (220 mM mannitol, 70 mM sucrose, 5 mM HEPES, pH 7.4). Varying concentrations of (R)-Chol-TPP are added, and after incubation at 25degC for 10-30 minutes, accumulation is measured by LC-MS/MS or by fluorescence if the compound contains a fluorophore. Membrane potential dependence is confirmed by addition of uncouplers like FCCP or CCCP, which abolish TPP accumulation.
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| Cell Assay |
For cellular uptake and mitochondrial localization studies, cells (e.g., HeLa, HEK293, primary neurons) are seeded on glass-bottom dishes or in 96-well plates. Cells are treated with (R)-Chol-TPP (0.1-10 uM) for 1-24 hours. For fluorescence microscopy, if the compound is fluorescent, live-cell imaging is performed. Alternatively, cells are co-stained with MitoTracker Red or Green to confirm mitochondrial co-localization. Colocalization is quantified using Pearson's correlation coefficient with confocal microscopy and image analysis software.
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| Animal Protocol |
For in vivo biodistribution studies, laboratory animals (typically mice or rats) are administered (R)-Chol-TPP intravenously (IV), intraperitoneally (IP), or orally (PO) at doses of 0.1-10 mg/kg. At various time points post-dosing (e.g., 0.5, 2, 6, 24 hours), animals are euthanized, and tissues (liver, heart, kidney, brain, lung, spleen) are collected. Tissues are homogenized, and compound concentrations are measured by LC-MS/MS to assess tissue distribution. Mitochondria are isolated from these tissues for subcellular localization analysis.
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| ADME/Pharmacokinetics |
TPP-conjugated compounds typically have high plasma protein binding (>95%) and extensive tissue distribution due to their lipophilic nature. Volume of distribution (Vd) is expected to be large (>10 L/kg), reflecting accumulation in tissues. Due to the permanent positive charge of the TPP cation, oral bioavailability is generally low, and intravenous or intraperitoneal administration is preferred for in vivo studies. Plasma half-life can be prolonged due to distribution into tissues. Detailed PK parameters for (R)-Chol-TPP are not publicly available.
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| Toxicity/Toxicokinetics |
As a chemical research tool, comprehensive toxicity data for (R)-Chol-TPP is not publicly available. TPP-based compounds as a class are generally well-tolerated at low concentrations in vitro (0.1-10 uM) but can be toxic at higher concentrations due to disruption of mitochondrial membrane potential. In vivo, the safety profile depends on the specific cargo. Standard safety precautions for handling chemicals apply. The compound is not intended for human therapeutic use. No acute or chronic toxicity data is available.
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| References | |
| Additional Infomation |
(R)-Chol-TPP is a research-grade chemical tool for mitochondrial biology studies. The TPP moiety is widely used for mitochondrial targeting of various cargoes including antioxidants (MitoQ, MitoTEMPO), imaging agents, and drugs. Mitochondrial cholesterol trafficking is an active area of research in steroidogenesis, neurodegenerative diseases (particularly Niemann-Pick type C disease), metabolic syndrome, and cancer biology. This compound is for research use only, not FDA-approved, and has not entered clinical trials.
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| Molecular Formula |
C55H78BRO5P
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|---|---|
| Molecular Weight |
930.08
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| Appearance |
White to off-white solid powder
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~107.52 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 | 1.0752 mL | 5.3759 mL | 10.7518 mL | |
| 5 mM | 0.2150 mL | 1.0752 mL | 2.1504 mL | |
| 10 mM | 0.1075 mL | 0.5376 mL | 1.0752 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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