| 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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| Targets |
Ispronicline is a selective agonist of the α4β2 nicotinic acetylcholine receptor (nAChR). This receptor subtype is widely expressed in the brain and is involved in cognitive function, attention, and neuroprotection. By activating this receptor, Ispronicline modulates neurotransmitter release and enhances cholinergic signaling.
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| ln Vitro |
In vitro, Ispronicline acts as a potent and selective agonist at the α4β2 nAChR. Its ability to modulate this receptor makes it a valuable tool for studying the role of nicotinic signaling in cognition and neuroprotection.
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| ln Vivo |
Ispronicline (10-20 mg/kg; subcutaneous injection) stimulates c-Fos expression in specific regions of the rat forebrain [1]. The pharmacokinetics of isopronicline (half-life in rats is 2 hours) stand in stark contrast to the long-lasting effects in working memory (18 hours to 2 days) [2].
In vivo, Ispronicline has been studied for its potential therapeutic effects in various medical conditions, including Alzheimer's disease, schizophrenia, and attention-deficit/hyperactivity disorder (ADHD). It has been investigated in clinical trials for its cognitive-enhancing and neuroprotective properties. |
| Enzyme Assay |
α4β2 nAChR binding affinity is determined using radioligand binding assays. Membrane preparations from cells expressing the receptor are incubated with varying concentrations of Ispronicline and a radiolabeled ligand. The Ki value is calculated from competitive binding curves.
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| Cell Assay |
Functional activity is assessed in cells expressing the α4β2 nAChR. The compound's ability to stimulate ion flux or modulate neurotransmitter release is measured. A dose-response curve is generated, and the EC50 is calculated.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat, body weight 180-200 g[1]
Doses: 10 and 30 mg/kg Route of Administration: subcutaneous injection Experimental Results: c-Fos was induced in the medial paraventricular nucleus of the hypothalamus. Treatment with 30 mg/kg isopronicline (but not 10 mg/kg) Dramatically increased the number of c-Fos immunoreactive cells in the medial parvocellular part of the paraventricular nucleus (PVN) compared with controls. In vivo efficacy is evaluated in animal models of cognitive impairment or neurological disease. Ispronicline is administered systemically, and cognitive function, neuroprotection, and other behavioral outcomes are assessed. |
| ADME/Pharmacokinetics |
As a small molecule, Ispronicline is expected to be orally bioavailable and to cross the blood-brain barrier. Its pharmacokinetic properties are consistent with a CNS-active drug. It has been investigated in clinical trials, indicating favorable pharmacokinetics.
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| Toxicity/Toxicokinetics |
As a nAChR agonist, potential toxicities may include nausea, dizziness, and other cholinergic side effects. However, its selectivity for the α4β2 subtype may reduce some side effects associated with non-selective nicotinic agonists.
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| References | |
| Additional Infomation |
Ispronicline is being investigated in the clinical trial NCT00109564 (Safety and efficacy study of Ispronicline (TC-1734-112) in subjects with age-related memory impairment (AAMI).
Ispronicline is a research compound that has been investigated in clinical trials for the treatment of Alzheimer's disease, schizophrenia, and ADHD. Its cognitive-enhancing and neuroprotective properties make it a promising candidate for the treatment of neurological and psychiatric disorders. It is also known as AZD3480. |
| Molecular Formula |
C14H22N2O
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|---|---|
| Molecular Weight |
234.343
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| Exact Mass |
234.173
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| Elemental Analysis |
C, 71.76; H, 9.46; N, 11.95; O, 6.83
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| CAS # |
252870-53-4
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| Related CAS # |
252870-53-4;252870-54-5 (hemigalactarate);957106-98-8 (phosphate);957107-01-6 (citrate);
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| PubChem CID |
9824145
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| Appearance |
Colorless to light yellow oily liquid
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| LogP |
3.27
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
17
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| Complexity |
228
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O(C1=C([H])N=C([H])C(=C1[H])/C(/[H])=C(\[H])/C([H])([H])[C@]([H])(C([H])([H])[H])N([H])C([H])([H])[H])C([H])(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
RPCVIAXDAUMJJP-PZBABLGHSA-N
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| InChi Code |
InChI=1S/C14H22N2O/c1-11(2)17-14-8-13(9-16-10-14)7-5-6-12(3)15-4/h5,7-12,15H,6H2,1-4H3/b7-5+/t12-/m0/s1
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| Chemical Name |
(E,2S)-N-methyl-5-(5-propan-2-yloxypyridin-3-yl)pent-4-en-2-amine
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| Synonyms |
AZD-3480 TC1734AZD 3480 TC-1734 AZD3480 Ispronicline
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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 (~426.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.67 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 (10.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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 (10.67 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 | 4.2673 mL | 21.3365 mL | 42.6730 mL | |
| 5 mM | 0.8535 mL | 4.2673 mL | 8.5346 mL | |
| 10 mM | 0.4267 mL | 2.1337 mL | 4.2673 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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