| Targets |
NSI-189 is a stimulator of neurogenesis of human hippocampus-derived neural stem cells. Its mechanism of action is not fully understood, but it is known to stimulate the proliferation and differentiation of neural stem cells, leading to the formation of new neurons. It is being investigated for a range of conditions, including major depressive disorder (MDD), post-traumatic stress disorder (PTSD), Alzheimer's disease, and age-related cognitive problems.
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| ln Vitro |
In vitro, NSI-189 stimulates the neurogenesis of human hippocampus-derived neural stem cells. It promotes the proliferation and differentiation of these cells into neurons. This activity is believed to be the basis for its antidepressant and procognitive effects. It also exhibits neuroprotective effects.
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| ln Vivo |
In vivo, NSI-189 has shown efficacy in preclinical models of depression and cognitive impairment. It stimulates neurogenesis in the hippocampus, which is thought to be a key mechanism for its antidepressant effects. It exhibits neuroprotective effects in a streptozotocin-induced diabetic mouse model. It is also being investigated for its potential in treating PTSD and age-related cognitive decline.
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| Enzyme Assay |
In vitro neurogenesis assays for NSI-189 are performed using human hippocampus-derived neural stem cells (hNSCs). Cells are cultured in neurobasal medium and treated with varying concentrations of the compound. The number of neurons formed is quantified by immunofluorescence staining for neuronal markers like β-III tubulin or NeuN, and the rate of proliferation is measured.
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| Cell Assay |
In vitro cell-based assays for NSI-189 are often performed using neural stem cells or neuronal cell lines. Cells are treated with the compound, and the effects on cell proliferation (e.g., by BrdU incorporation) and differentiation (e.g., by measuring the expression of neuronal markers) are assessed.
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| Animal Protocol |
In vivo animal studies for NSI-189 have been conducted in rodent models of depression, such as the chronic mild stress model or the forced swim test. The compound is administered orally or intraperitoneally, and its effects on depressive-like behaviors are measured. Its effects on neurogenesis are confirmed by immunohistochemical staining for BrdU and neuronal markers in brain tissue.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic properties of NSI-189 Phosphate, such as half-life and bioavailability, are not detailed in the available literature. It is a small molecule that is likely to have good oral bioavailability and be able to cross the blood-brain barrier. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for NSI-189 Phosphate are not provided in the available text. As a research compound, it is intended for laboratory use only and is not for human therapeutic use. Safety precautions should be followed when handling this compound.
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| Additional Infomation |
NSI-189 Phosphate is a novel neurogenic molecule that stimulates the neurogenesis of human hippocampus-derived neural stem cells. It has antidepressant, procognitive, and neuroprotective activities. This product is for research use only.
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| Exact Mass |
464.219
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|---|---|
| CAS # |
1270138-41-4
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| PubChem CID |
50922680
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| Appearance |
White to off-white solid powder
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| LogP |
2.517
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
491
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LWHMGALTTIYPJU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H30N4O.H3O4P/c1-18(2)10-12-24-21-20(9-6-11-23-21)22(27)26-15-13-25(14-16-26)17-19-7-4-3-5-8-19;1-5(2,3)4/h3-9,11,18H,10,12-17H2,1-2H3,(H,23,24);(H3,1,2,3,4)
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| Chemical Name |
(4-benzylpiperazin-1-yl)-[2-(3-methylbutylamino)pyridin-3-yl]methanone;phosphoric acid
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| Synonyms |
NSI189 Phosphate NSI-189 Phosphate NSI 189 Phosphate
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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) |
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.) |
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.
Products are for research use only; We do not sell to patients
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