| 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 |
FGIN 1-43 targets the mitochondrial diazepam binding inhibitor (DBI) receptor, also known as the translocator protein (TSPO). This receptor is involved in the production of neurosteroids, which modulate GABA-A receptor function. By binding to the DBI receptor, FGIN 1-43 induces neurosteroid production, which enhances GABAergic neurotransmission. The compound is of interest in drug discovery as a potential candidate for targeted therapies in oncology and neurology. Its mechanism involves disrupting receptor interactions and downstream signaling pathways.
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| ln Vitro |
In vitro, FGIN 1-43 acts as an effective and specific ligand for the mitochondrial DBI receptor. The compound's binding to this receptor induces neurosteroid production. As a TSPO ligand, it modulates steroidogenesis in mitochondrial membranes. The compound has been studied for its potential in anti-anxiety research. However, detailed in vitro activity data including binding affinity (Ki or IC₅₀) are not extensively published in the available literature. Its specificity for the DBI receptor suggests minimal off-target effects.
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| ln Vivo |
In vivo, FGIN 1-43 has been studied for its anti-anxiety effects through induction of neurosteroid production and enhancement of GABA transmission. By binding to the mitochondrial DBI receptor, the compound promotes the synthesis of neuroactive steroids that positively modulate GABA-A receptors, producing anxiolytic-like effects. The compound's ability to cross the blood-brain barrier is essential for its central nervous system activity. However, detailed in vivo efficacy data from animal models are not extensively published in the available literature.
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| Enzyme Assay |
In vitro receptor binding assays for FGIN 1-43 involve radioligand binding studies using mitochondrial membranes or cells expressing the DBI receptor (TSPO). The compound's binding affinity is determined by competition binding assays using labeled ligands such as [³H]PK11195. Specific binding is calculated by subtracting non-specific binding (determined in the presence of excess unlabeled ligand). IC₅₀ or Ki values are calculated from displacement curves. Neurosteroid production can be measured by radioimmunoassay or ELISA.
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| Cell Assay |
In vitro cellular assays for FGIN 1-43 typically involve evaluation of neurosteroid production in cell lines expressing TSPO. Cells are treated with the compound and steroid production is measured using immunoassays or mass spectrometry. For GABAergic activity assessment, electrophysiological recordings in neuronal cultures can be used to measure GABA-A receptor currents. Cytotoxicity may be assessed in relevant cell lines using MTT or similar assays. The compound is typically dissolved in DMSO for cell culture applications.
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| Animal Protocol |
In vivo animal experiments for FGIN 1-43 would typically involve rodent models of anxiety or neurological disorders. The compound is administered via intraperitoneal or oral routes, and behavioral assays such as elevated plus maze, open field test, or light-dark box are used to evaluate anxiolytic effects. Neurosteroid levels in brain tissue can be measured to confirm target engagement. However, detailed experimental protocols and results are not extensively published in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of FGIN 1-43 are characteristic of lipophilic small molecules. The compound has a molecular weight of 487.50 g/mol and molecular formula C₂₈H₃₆Cl₂N₂O. As a lipophilic compound with two chlorine atoms, it is expected to have good blood-brain barrier penetration, which is essential for its central nervous system activity. The compound is typically dissolved in DMSO for experimental use. Storage: powder at -20°C for 3 years or 4°C for 2 years; in solvent at -80°C for 6 months or -20°C for 1 month.
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| Toxicity/Toxicokinetics |
The toxicological profile of FGIN 1-43 is not extensively documented. The compound is a research chemical used for target validation and drug discovery. As a TSPO ligand, its toxicity profile would be evaluated in the context of therapeutic development. Comprehensive toxicological evaluations including acute toxicity, genotoxicity, and repeated-dose studies have not been reported in the available literature. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
2-[5-chloro-2-(4-chlorophenyl)-1H-indole-3-yl]-N,N-dihexylacetamide is a phenylindole.
FGIN 1-43 (CAS# 145040-29-5, molecular formula C₂₈H₃₆Cl₂N₂O, molecular weight 487.50) is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor. It induces neurosteroid production and enhances GABA transmission, with potential applications in anti-anxiety research. No clinical trials or regulatory approvals have been identified. Storage: powder at -20°C for 3 years or 4°C for 2 years. |
| Molecular Formula |
C28H36CL2N2O
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|---|---|
| Molecular Weight |
487.50424
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| Exact Mass |
486.22
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| CAS # |
145040-29-5
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| PubChem CID |
3995234
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| Appearance |
White to off-white solid powder
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| Density |
1.143g/cm3
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| Boiling Point |
648.5ºC at 760 mmHg
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| Flash Point |
346ºC
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| Vapour Pressure |
1.05E-16mmHg at 25°C
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| Index of Refraction |
1.579
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| LogP |
8.673
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
33
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| Complexity |
554
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=CC=C2C(C(CC(N(CCCCCC)CCCCCC)=O)=C(C3C=CC(Cl)=CC=3)N2)=C1
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| InChi Key |
XTZUPNNVXIMWAR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H36Cl2N2O/c1-3-5-7-9-17-32(18-10-8-6-4-2)27(33)20-25-24-19-23(30)15-16-26(24)31-28(25)21-11-13-22(29)14-12-21/h11-16,19,31H,3-10,17-18,20H2,1-2H3
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| Chemical Name |
2-[5-chloro-2-(4-chlorophenyl)-1H-indol-3-yl]-N,N-dihexylacetamide
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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 (205.13 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 | 2.0513 mL | 10.2564 mL | 20.5128 mL | |
| 5 mM | 0.4103 mL | 2.0513 mL | 4.1026 mL | |
| 10 mM | 0.2051 mL | 1.0256 mL | 2.0513 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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