| Size | Price | Stock | Qty |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Leteprinim potassium targets neurotrophic factors, including brain-derived neurotrophic factor (BDNF) and nerve growth factor (NGF), as well as the antioxidant enzymes heme-oxygenase 1 and 2. By inducing the production of BDNF and NGF, Leteprinim potassium promotes the survival, growth, and differentiation of neurons. This neurotrophic activity is crucial for its neuroprotective effects. The compound also increases the expression of heme-oxygenase 1 and 2, which are enzymes that provide cellular protection against oxidative stress by degrading pro-oxidant heme to biliverdin, carbon monoxide, and free iron. This antioxidant effect may contribute to its ability to reduce glutamate toxicity. Leteprinim potassium's mechanism of action involves the modulation of multiple pathways that support neuronal health and survival. The compound's ability to cross the blood-brain barrier and its unique transport mechanisms (nonsaturable influx, saturable efflux) are important for its pharmacokinetic profile and its effects on the central nervous system. Leteprinim potassium is a cognitive enhancer and neurotrophic agent.
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| ln Vitro |
Leteprinim potassium demonstrates potent in vitro activity as a neurotrophic and neuroprotective agent. It enhances nerve growth factor (NGF) at concentrations of 10 and 100 µM. In cultured hippocampal neurons, Leteprinim potassium reduces glutamate toxicity, indicating its ability to protect neurons from excitotoxic damage. The compound increases heme-oxygenase 1 and 2 mRNA levels, which play a role in cellular defense against reactive oxygen species (ROS). This antioxidant effect may contribute to its neuroprotective activity. These in vitro findings establish Leteprinim potassium as a promising agent for the treatment of neurodegenerative diseases.
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| ln Vivo |
In young rats with hypoxic-ischemic brain damage, leprinine potassium (60 mg/kg; IP; single dose) dramatically lowers the amount of apoptotic neurons [1].
Leteprinim potassium has been shown to have neuroprotective activity and to enhance working memory in animal models. It is being studied for its potential in treating Alzheimer's disease and spinal cord injury. The compound's ability to induce the production of BDNF and NGF in vivo likely underlies its beneficial effects on cognition and neuronal survival. Further in vivo studies are needed to fully characterize its efficacy in different disease models. |
| Enzyme Assay |
The in vitro enzyme/receptor binding (non-cellular) assay for Leteprinim potassium is not a typical enzyme inhibition assay, as its primary mechanism involves the modulation of gene expression rather than direct enzyme inhibition. However, its effects on gene expression can be studied in cell-free systems. For example, the compound's ability to induce BDNF or NGF mRNA expression can be assessed using a reporter gene assay or by measuring mRNA levels in vitro. These assays are important for understanding the compound's mechanism of action at the molecular level.
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| Cell Assay |
The in vitro cellular assay for Leteprinim potassium typically involves evaluating its neuroprotective and neurotrophic effects on neuronal cell cultures. In a typical assay, primary neurons or neuronal cell lines are treated with Leteprinim potassium, and the expression of BDNF, NGF, or heme-oxygenase 1 and 2 mRNA is measured by qPCR. To assess neuroprotection, neurons are treated with glutamate in the presence or absence of Leteprinim potassium, and neuronal survival is measured using an MTT or similar assay. The results show that Leteprinim potassium induces the expression of neurotrophic factors and protects neurons from glutamate toxicity. These cellular assays are crucial for confirming the compound's mechanism of action and for evaluating its potency and efficacy in a relevant biological context.
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| Animal Protocol |
Animal/Disease Models: Wistar young rats (hypoxic-ischemic brain injury induced by permanent unilateral carotid artery ligation) [1]
Doses: 60 mg/kg Route of Administration: IP; Single dose Experimental Results: compared with normal saline treatment group , the number of retained neurons in the hippocampal CA1, CA3 areas and dentate gyrus of the left hemisphere increased Dramatically. In the right hemisphere, compared with the saline group, the neuron density in the hippocampal CA1, CA2, CA3 areas and dentate gyrus was Dramatically increased in the netrofin-treated group. The in vivo animal experimental protocol for Leteprinim potassium typically involves the use of rodent models of neurological diseases. In a typical study, Leteprinim potassium is administered to animals, and its effects on cognitive function, neuronal survival, and neurotrophic factor expression are assessed. For example, in a model of Alzheimer's disease, the compound's ability to improve memory and reduce amyloid pathology could be evaluated. In a model of spinal cord injury, its ability to promote neuronal regeneration and functional recovery could be assessed. The compound's transport mechanisms (nonsaturable influx, saturable efflux) are also studied in vivo. These in vivo models are essential for demonstrating the compound's therapeutic potential. |
| ADME/Pharmacokinetics |
Leteprinim potassium enters the brain by a nonsaturable influx mechanism and leaves by a saturable efflux mechanism. This unique transport profile influences its pharmacokinetics and its ability to reach its targets in the central nervous system. The compound has a molecular weight of 365.39. Further PK studies are needed to fully characterize its absorption, distribution, metabolism, and excretion (ADME) profile.
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| Toxicity/Toxicokinetics |
Specific toxicity (toxicology) data for Leteprinim potassium are not reported in the available literature. However, as a neuroprotective agent, it is expected to have a favorable safety profile. Comprehensive toxicological assessments would be necessary to fully evaluate its safety for clinical development.
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| References |
[1]. Effects of neotrofin on neonatal hypoxic ischemic brain injury. Neurosci Lett. 2011 Nov 14;505(2):205-10.
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| Additional Infomation |
Leteprinim potassium is also known as AIT-082 and SPI-205. It is a synthetic purine derivative with neuroprotective and neurotrophic effects. Leteprinim potassium induces the production of BDNF and NGF, and increases heme-oxygenase 1 and 2 mRNA levels. It reduces glutamate toxicity in cultured hippocampal neurons. The compound enters the brain by a nonsaturable influx mechanism and leaves by a saturable efflux mechanism. It has a molecular formula of C15H12KN5O4 and a molecular weight of 365.39.
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| Molecular Formula |
C15H12N5O4-.K+
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|---|---|
| Molecular Weight |
365.38518
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| Exact Mass |
365.053
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| Elemental Analysis |
C, 49.31; H, 3.31; K, 10.70; N, 19.17; O, 17.51
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| CAS # |
192564-13-9
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| Related CAS # |
138117-50-7 (Leteprinim free base);
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| PubChem CID |
135413527
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
550
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[K+].O=C(C1C=CC(NC(CCN2C=NC3C(N=CNC2=3)=O)=O)=CC=1)[O-]
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| InChi Key |
MICLTPPSCUXHJT-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C15H13N5O4.K/c21-11(19-10-3-1-9(2-4-10)15(23)24)5-6-20-8-18-12-13(20)16-7-17-14(12)22;/h1-4,7-8H,5-6H2,(H,19,21)(H,23,24)(H,16,17,22);/q;+1/p-1
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| Chemical Name |
potassium;4-[3-(6-oxo-1H-purin-9-yl)propanoylamino]benzoate
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| Synonyms |
Leteprinim Potassium Salt; Leteprinim potassium; Neotrofin; AIT 082 potassium; AIT-082; SPI-205; AIT082; SPI205; AIT 082; SPI 205; 192564-13-9;
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7368 mL | 13.6840 mL | 27.3680 mL | |
| 5 mM | 0.5474 mL | 2.7368 mL | 5.4736 mL | |
| 10 mM | 0.2737 mL | 1.3684 mL | 2.7368 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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