| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
TSPO ligand-1 targets the translocator protein (TSPO), a mitochondrial outer membrane protein. TSPO is involved in various cellular functions including cholesterol transport and mitochondrial function. By binding to TSPO, the compound can modulate mitochondrial autophagy (mitophagy) and promote targeted mitochondrial renewal. TSPO ligand-1 is also a sensitive biomarker of brain damage and neurodegeneration.
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| ln Vitro |
The selective activation of male C57Bl6/N mouse neurons was used to induce an increase in the expression of the TSPO ligand-1 gene. Additionally, increased TSPO levels in adult mice are also a result of neuronal activation in both physiological and psychopharmacological settings [2]. As the sole indicator of glial cell activity in Alzheimer's disease, TSPO ligand-1 can be used to monitor the development of new nerve cells [3]. In the MA-10 Leydig cell line, TSPO ligand-1 can control mitochondrial fatty acid oxidation (FAO), which in turn affects mitochondrial energy homeostasis [4].
In vitro, TSPO ligand-1 binds to AUTAC4 and regulates mitochondrial autophagy (mitophagy) to promote targeted mitochondrial renewal. It is a mitochondrial outer membrane transmembrane structural domain protein. The compound's ability to modulate mitophagy makes it a valuable tool for studying mitochondrial quality control. |
| ln Vivo |
Specific in vivo data for TSPO ligand-1 are limited. The compound has potential for therapeutic applications in neuroinflammatory and neurodegenerative conditions, including Alzheimer's disease and Parkinson's disease. However, detailed in vivo efficacy studies are not extensively reported. The compound is primarily used as a research tool.
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| Enzyme Assay |
In vitro binding assays for TSPO ligand-1 measure its affinity for TSPO. Radioligand binding assays or surface plasmon resonance (SPR) can be used to characterize the compound's interaction with TSPO. The compound's ability to modulate mitophagy can be assessed in cell-based assays by measuring mitochondrial mass and function.
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| Cell Assay |
Cell-based assays for TSPO ligand-1 are conducted in cell lines to assess its effects on mitophagy. Cells are treated with the compound, and mitochondrial autophagy is assessed by measuring mitochondrial mass, mitophagy markers, and mitochondrial function. These assays characterize the compound's ability to promote targeted mitochondrial renewal.
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| Animal Protocol |
In vivo animal experiments with TSPO ligand-1 have not been extensively documented. The compound could potentially be used in models of neurodegenerative diseases to assess its effects on mitochondrial function and neuroprotection. Specific protocols are not available.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TSPO ligand-1 are not extensively characterized. The compound has a molecular formula of C16H10ClNO2 and a molecular weight of 283.71. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year. Specific data on absorption, distribution, metabolism, and excretion are not available.
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| Toxicity/Toxicokinetics |
Safety and toxicology data for TSPO ligand-1 are limited. The compound is for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling the compound. No specific toxicity data are available.
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| References |
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| Additional Infomation |
TSPO ligand-1 has CAS number 4560-08-1, molecular formula C16H10ClNO2, and molecular weight 283.71. It is a ligand of AUTAC4 that can be used in the synthesis of PROTACs. It regulates mitophagy and promotes targeted mitochondrial renewal. Not for human use; for research purposes only.
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| Molecular Formula |
C16H10CLNO2
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|---|---|
| Molecular Weight |
283.709103107452
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| Exact Mass |
283.04
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| CAS # |
4560-08-1
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| PubChem CID |
12589400
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| Appearance |
Light yellow to green yellow solid powder
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
392
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC(C(C1C2C=CC=CC=2NC=1C1C=CC=CC=1)=O)=O
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| InChi Key |
DREHVYWKTXGDBS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H10ClNO2/c17-16(20)15(19)13-11-8-4-5-9-12(11)18-14(13)10-6-2-1-3-7-10/h1-9,18H
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| Chemical Name |
2-oxo-2-(2-phenyl-1H-indol-3-yl)acetyl chloride
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 | 3.5247 mL | 17.6236 mL | 35.2473 mL | |
| 5 mM | 0.7049 mL | 3.5247 mL | 7.0495 mL | |
| 10 mM | 0.3525 mL | 1.7624 mL | 3.5247 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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