| 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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| Other Sizes |
| Targets |
FGIN 1-27 targets the translocator protein (TSPO), also known as the peripheral benzodiazepine receptor (PBR). It binds to TSPO with high affinity (Ki = 5.0 nM). TSPO is a mitochondrial membrane protein involved in cholesterol transport and neurosteroid biosynthesis. By binding to TSPO, FGIN 1-27 stimulates the production of neurosteroids such as allopregnanolone, which have anxiolytic, anticonvulsant, and neuroprotective effects. The compound does not bind to GABAA receptors.
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| ln Vitro |
FGIN 1-27 is a high-affinity ligand for TSPO (Ki = 5.0 nM). It stimulates neurosteroid biosynthesis by facilitating cholesterol transport into mitochondria. The compound can cross the blood-brain barrier. FGIN 1-27 inhibits the onset of isoniazid-induced convulsions, demonstrating anticonvulsant activity. It also has anxiolytic properties. The compound has been shown to downregulate the expression of RORγt target genes. FGIN 1-27 does not bind to GABAA receptors.
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| ln Vivo |
FGIN 1-27 inhibits the onset of isoniazid-induced convulsions in animal models, demonstrating anticonvulsant activity. The compound can cross the blood-brain barrier and stimulate neurosteroid biosynthesis in vivo. It has anxiolytic properties. The compound's ability to increase neurosteroid levels in the brain contributes to its anticonvulsant and anxiolytic effects. Specific dosing regimens and efficacy data would be determined from preclinical studies.
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| Enzyme Assay |
The in vitro receptor binding assay for FGIN 1-27 typically involves measuring its affinity for TSPO using radioligand binding. Membrane preparations from tissues or cells expressing TSPO are incubated with varying concentrations of FGIN 1-27 (typically 0.001-100 μM) and a radiolabeled ligand such as [3H]PK11195. The binding affinity (Ki) is determined by competition binding analysis. The compound is dissolved in DMSO and diluted in assay buffer. Functional assays involve measuring TSPO-mediated cholesterol transport or neurosteroid production in mitochondrial preparations.
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| Cell Assay |
In vitro cellular assays for FGIN 1-27 typically involve treating TSPO-expressing cells (such as glial cells or steroidogenic cells) with the compound at concentrations ranging from 0.001 to 10 μM. Neurosteroid production (such as pregnenolone and allopregnanolone) is measured by radioimmunoassay or mass spectrometry. Cellular viability and mitochondrial function are assessed using standard assays. The compound is dissolved in DMSO as a stock solution and diluted in cell culture medium, with DMSO-only treated cells serving as controls.
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| Animal Protocol |
In vivo animal studies for FGIN 1-27 typically involve administration to rodents via intraperitoneal or intravenous injection at doses ranging from 0.1 to 10 mg/kg. Anticonvulsant activity is assessed using models such as isoniazid-induced seizures. Anxiolytic effects are evaluated using behavioral tests such as the elevated plus maze or light-dark box. Neurosteroid levels in brain tissue are measured by mass spectrometry. The compound's ability to cross the blood-brain barrier is assessed by measuring brain concentrations.
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| ADME/Pharmacokinetics |
FGIN 1-27 has a molecular weight of 436.62 g/mol and formula C28H37FN2O. The compound can cross the blood-brain barrier. It is typically stored at -20°C for powder and -80°C for solvent. The compound is soluble in DMSO and other organic solvents. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would require experimental determination. The compound's ability to penetrate the blood-brain barrier supports its use in neurological studies.
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| Toxicity/Toxicokinetics |
Toxicity data for FGIN 1-27 are not extensively reported. The compound is intended for research use only and is not approved for human therapeutic applications. Standard preclinical toxicity assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, and assessment of off-target effects. The compound's mechanism of action involves neurosteroid biosynthesis, which could have physiological effects at high doses. Appropriate safety precautions should be taken when handling.
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| References | |
| Additional Infomation |
2-[2-(4-fluorophenyl)-1H-indole-3-yl]-N,N-dihexylacetamide is a phenylindole.
FGIN 1-27 (CAS 142720-24-9) is an indoleacetamide that acts as a high-affinity ligand for the translocator protein (TSPO) with a Ki of 5.0 nM. It stimulates neurosteroid biosynthesis, can cross the blood-brain barrier, and inhibits isoniazid-induced convulsions. The compound has anxiolytic properties and does not bind to GABAA receptors. It is also known as N,N-dihexyl-2-(4-fluorophenyl)indole-3-acetamide. FGIN 1-27 is not approved for clinical use. |
| Molecular Formula |
C28H37N2OF
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|---|---|
| Molecular Weight |
436.60458
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| Exact Mass |
436.289
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| CAS # |
142720-24-9
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| PubChem CID |
132496
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.073g/cm3
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| Boiling Point |
608.3ºC at 760mmHg
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| Flash Point |
321.7ºC
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| Vapour Pressure |
9.6E-15mmHg at 25°C
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| Index of Refraction |
1.562
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| LogP |
7.505
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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 |
13
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| Heavy Atom Count |
32
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| Complexity |
522
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC(C2=C(CC(N(CCCCCC)CCCCCC)=O)C3C(=CC=CC=3)N2)=CC=1
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| InChi Key |
VUWXAQFLTSBUDB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H37FN2O/c1-3-5-7-11-19-31(20-12-8-6-4-2)27(32)21-25-24-13-9-10-14-26(24)30-28(25)22-15-17-23(29)18-16-22/h9-10,13-18,30H,3-8,11-12,19-21H2,1-2H3
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| Chemical Name |
2-[2-(4-fluorophenyl)-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 |
| 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 (~229.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume 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 (5.73 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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 (5.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2904 mL | 11.4521 mL | 22.9043 mL | |
| 5 mM | 0.4581 mL | 2.2904 mL | 4.5809 mL | |
| 10 mM | 0.2290 mL | 1.1452 mL | 2.2904 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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