| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
monoamine transporter[1]
The primary molecular targets of Indatraline HCl are the serotonin transporter (SERT), dopamine transporter (DAT), and norepinephrine transporter (NET). It is a non-selective monoamine reuptake inhibitor with Ki values of 0.42 nM for SERT, 1.7 nM for DAT, and 5.8 nM for NET. By blocking these transporters, it increases synaptic concentrations of serotonin, dopamine, and norepinephrine. Additionally, Indatraline induces autophagy through AMPK activation and mTOR/S6K inhibition. The compound also inhibits smooth muscle cell proliferation independently of its monoamine transporter effects. |
|---|---|
| ln Vitro |
Indataline hydrochloride (0-5 μM; 24 hours; EGFP-LC3 stable cells) produces LC3 [1]. Indataline hydrochloride (1-10 μM; 24 hours; HeLa cells) induces EGFP-LC3 fluorescence in the cytoplasm [1]. Indataline hydrochloride (1-20 μM) inhibits smooth muscle cell growth with an IC50 of 15 μM. Indataline also promotes autophagy and modulates the AMPK/mTOR/S6K signaling axis [1].
In vitro, Indatraline HCl (0-5 μM; 24 hours) induces concentration-dependent conversion of LC3 in EGFP-LC3 stable cells. In HeLa cells, Indatraline (1-10 μM; 24 hours) increases EGFP-LC3 fluorescent vacuoles in the cytoplasm in a concentration-dependent manner. Indatraline (1-20 μM) inhibits smooth muscle cell proliferation with an IC50 of 15 μM. It induces autophagy through AMPK/mTOR/S6K signaling axis modulation. Western blot analysis in HeLa cells treated with 0-5 μM Indatraline for 24 hours shows concentration-dependent LC3 conversion. |
| ln Vivo |
Inhibiting smooth muscle cell neointimal accumulation is achieved by indatraline hydrochloride (2 μM) [1].
In vivo, Indatraline (2 μM) inhibits neointimal accumulation of smooth muscle cells. In animal models of restenosis, the compound reduces vascular smooth muscle cell proliferation and neointima formation. Its effects on monoamine transporters produce behavioral effects similar to cocaine in rodent models. The compound's autophagy-inducing activity may contribute to its effects on vascular remodeling. In vivo pharmacokinetic studies would determine brain penetration and appropriate dosing for central nervous system effects. |
| Enzyme Assay |
For non-cellular receptor binding assays, Indatraline HCl binding to monoamine transporters is measured using radioligand binding assays with membranes from cells expressing recombinant human SERT, DAT, or NET. Radiolabeled ligands such as [3H]paroxetine for SERT, [3H]WIN 35,428 for DAT, and [3H]nisoxetine for NET are used as tracers. Membranes are incubated with radioligand and increasing concentrations of Indatraline, and bound radioactivity is quantified by scintillation counting. Ki values are calculated using the Cheng-Prusoff equation.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HeLa cells Tested Concentrations: 0~5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Made the concentration-dependent conversion of LC3. Immunofluorescence[1] Cell Types: EGFP-LC3 stable cells Tested Concentrations: 1~10 μM Incubation Duration: 24 hrs (hours) Experimental Results: EGFP-LC3 fluorescent vacuoles increased concentration-dependently in the cytoplasm. In vitro cell experiments with Indatraline HCl use HeLa cells, EGFP-LC3 stable cells, or smooth muscle cells. Cells are cultured in standard medium and treated with varying concentrations of Indatraline (typically 0-20 μM) for 24 hours. Autophagy is assessed by Western blotting for LC3 conversion and immunofluorescence for EGFP-LC3 vacuoles. Smooth muscle cell proliferation is measured by MTT or BrdU incorporation assays. AMPK, mTOR, and S6K phosphorylation are assessed by Western blotting to evaluate signaling pathway modulation. |
| Animal Protocol |
In vivo animal experiments with Indatraline HCl use rodent models for restenosis or behavioral studies. For restenosis models, vascular injury is induced by balloon catheterization, and animals receive Indatraline (2 μM) locally or systemically. Neointima formation is assessed by histomorphometry. For behavioral studies, locomotor activity and drug discrimination tests assess monoamine transporter inhibition effects. Pharmacokinetic studies determine plasma and brain concentrations of Indatraline to guide dose selection.
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| References |
| Molecular Formula |
C16H16CL3N
|
|---|---|
| Molecular Weight |
328.66
|
| Exact Mass |
327.035
|
| CAS # |
96850-13-4
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| Related CAS # |
cis-Indatraline hydrochloride;86939-08-4
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| PubChem CID |
10314472
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| Appearance |
White to off-white solid
|
| LogP |
5.982
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| tPSA |
12.03
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
309
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| Defined Atom Stereocenter Count |
2
|
| SMILES |
N([C@H]1C2C=CC=CC=2[C@H](C2C=CC(Cl)=C(Cl)C=2)C1)C.Cl
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| InChi Key |
QICQDZXGZOVTEF-MELYUZJYSA-N
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| InChi Code |
InChI=1S/C16H15Cl2N.ClH/c1-19-16-9-13(11-4-2-3-5-12(11)16)10-6-7-14(17)15(18)8-10/h2-8,13,16,19H,9H2,1H31H/t13-,16+/m0./s1
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| Chemical Name |
(1R,3S)-3-(3,4-dichlorophenyl)-N-methyl-2,3-dihydro-1H-inden-1-amine hydrochloride
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| Synonyms |
Indatraline Hydrochloride Indatraline HCl salt Indatraline HCl
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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, 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 | 3.0427 mL | 15.2133 mL | 30.4266 mL | |
| 5 mM | 0.6085 mL | 3.0427 mL | 6.0853 mL | |
| 10 mM | 0.3043 mL | 1.5213 mL | 3.0427 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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