| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
BMT-124110 targets AAK1 (AP2 associated kinase 1), a kinase involved in clathrin-mediated endocytosis and synaptic vesicle recycling. It is a potent and selective AAK1 inhibitor with an IC50 of 0.9 nM. BMT-124110 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 17 nM and Cyclin G-associated kinase (GAK) with an IC50 of 99 nM. AAK1 inhibition is being explored for the treatment of pain and neurodegenerative diseases.
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| ln Vitro |
The cellular IC50 of AAK1 in BMT-124110 is 3.2±1.4 nM [1].
In vitro, BMT-124110 demonstrates potent inhibition of AAK1 with an IC50 of 0.9 nM. It also inhibits BIKE (IC50 = 17 nM) and GAK (IC50 = 99 nM). The compound shows antinociceptive activity in cellular models. It is used to study the role of AAK1 in pain signaling, synaptic function, and endocytosis. The compound's selectivity for AAK1 over other kinases makes it a valuable tool for studying AAK1-mediated pathways. |
| ln Vivo |
In 10 out of 14 mice, the addition of BMT-124110 directly to the spinal cord via microiontophoresis caused a decrease in saturation-induced activity [1].
In vivo, BMT-124110 shows antinociceptive activity, suggesting potential for pain treatment. The compound's AAK1 inhibitory activity may affect synaptic function and neurotransmission. In vivo studies typically assess the analgesic effects of BMT-124110 in rodent pain models. The compound's effects on endocytosis and neuronal signaling are evaluated. Further studies are needed to fully characterize its in vivo efficacy and safety profile. |
| Enzyme Assay |
Non-cellular enzyme/receptor binding assay protocols for BMT-124110 involve measuring AAK1 inhibition. AAK1 kinase activity is assessed using kinase assays with recombinant AAK1 and peptide substrates. The IC50 of 0.9 nM is determined by measuring the inhibition of kinase activity at various concentrations of the compound. Selectivity assays against other kinases (including BIKE and GAK) are performed to confirm specificity. Binding studies can be performed using SPR or ITC.
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| Cell Assay |
Cellular assay protocols for BMT-124110 involve treating cells with the compound. Cells are incubated with various concentrations of BMT-124110 for defined periods. AAK1 inhibition is assessed by measuring phosphorylation of AAK1 substrates by western blot. Effects on endocytosis can be evaluated using transferrin uptake assays. Antinociceptive activity can be assessed in neuronal cell models. Cell viability assays are performed to evaluate cytotoxicity.
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| Animal Protocol |
In vivo animal experiment protocols for BMT-124110 typically involve rodent pain models. The compound is administered orally, intraperitoneally, or intravenously at various doses. Analgesic effects are assessed using behavioral tests such as the hot plate test, tail flick test, or formalin test. Tissue samples are collected for PK/PD analysis, including measurement of compound concentrations and assessment of AAK1 inhibition in tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of BMT-124110 have been characterized. As a small molecule (MW 369.46 g/mol), it is expected to have reasonable oral bioavailability. Further PK studies would be needed to fully characterize its absorption, distribution, metabolism, and excretion profile, including half-life (t½), maximum concentration (Cmax), and clearance (CL).
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| Toxicity/Toxicokinetics |
Toxicity of BMT-124110 has not been extensively reported. As a kinase inhibitor, it may affect normal cellular processes. Standard toxicological evaluation would include acute and sub-chronic toxicity studies in rodents, genotoxicity testing, and cardiovascular safety assessments. The compound is for research use only and not for human therapeutic applications.
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| References | |
| Additional Infomation |
BMT-124110 (CAS: 1679371-59-5) has a molecular formula of C21H27N3O3 and a molecular weight of 369.46 g/mol. It is a potent and selective AAK1 inhibitor with an IC50 of 0.9 nM. It shows antinociceptive activity and inhibits BIKE (IC50 = 17 nM) and GAK (IC50 = 99 nM). Chemical name: N-(8-{[(2S)-2-amino-2,4-dimethylpentyl]oxy}-5H-chromeno[3,4-c]pyridin-2-yl)acetamide. Purity is typically ≥98%. This product is for research use only.
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| Molecular Formula |
C₂₁H₂₇N₃O₃
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|---|---|
| Molecular Weight |
369.46
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| Exact Mass |
369.205
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| CAS # |
1679371-59-5
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| PubChem CID |
117953652
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
515
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)C[C@@](C)(COC1=CC2=C(C=C1)C3=CC(=NC=C3CO2)NC(=O)C)N
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| InChi Key |
OQMXEZIHZRSBOY-NRFANRHFSA-N
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| InChi Code |
InChI=1S/C21H27N3O3/c1-13(2)9-21(4,22)12-27-16-5-6-17-18-8-20(24-14(3)25)23-10-15(18)11-26-19(17)7-16/h5-8,10,13H,9,11-12,22H2,1-4H3,(H,23,24,25)/t21-/m0/s1
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| Chemical Name |
N-[8-[(2S)-2-amino-2,4-dimethylpentoxy]-5H-chromeno[3,4-c]pyridin-2-yl]acetamide
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| Synonyms |
BMT124110; BMT 124110
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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 | 2.7067 mL | 13.5333 mL | 27.0665 mL | |
| 5 mM | 0.5413 mL | 2.7067 mL | 5.4133 mL | |
| 10 mM | 0.2707 mL | 1.3533 mL | 2.7067 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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