| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
L-type calcium channel (CaV1.2).
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|---|---|
| ln Vitro |
MEM-1003 is a potent L-type Ca2+ channel antagonist. It blocks calcium influx through L-type calcium channels. The compound is brain-penetrant, allowing it to modulate calcium signaling in the central nervous system. It has been studied for its effects on eyeblink conditioning in older rabbits. MEM-1003 has potential applications in bipolar disorder and Alzheimer's disease research.
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| ln Vivo |
MEM-1003 has been evaluated in vivo for its efficacy in delay and trace eyeblink conditioning in older rabbits. The compound is brain-penetrant, enabling central nervous system activity. It has potential for the treatment of bipolar disorders and Alzheimer's disease. Further in vivo studies would be needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
In vitro receptor binding assays for L-type calcium channel antagonism use membrane preparations from cells expressing recombinant CaV1.2 channels or from brain tissue. Radiolabeled dihydropyridine ligands (e.g., [3H]nitrendipine) are used as tracers. MEM-1003 is incubated with membranes and radioligand at varying concentrations (typically 0.01 nM to 100 µM). Ki values are calculated from competition binding curves. Selectivity is assessed against other calcium channel subtypes.
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| Cell Assay |
In vitro cellular assays are performed using neuronal cell lines or primary neurons. Cells are treated with MEM-1003 at concentrations ranging from 0.01-100 µM. Intracellular calcium levels are measured using fluorescent dyes (e.g., Fura-2 or Fluo-4) following depolarization with high potassium or veratridine. Cell viability is monitored using MTT assays. Neurite outgrowth and synaptic plasticity can be assessed in appropriate cell models. Electrophysiological recordings (patch-clamp) measure calcium channel currents.
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| Animal Protocol |
In vivo efficacy is evaluated in rabbit models of eyeblink conditioning. MEM-1003 is administered at appropriate doses and routes. Acquisition and retention of conditioned responses are measured. For bipolar disorder studies, appropriate animal models (e.g., amphetamine-induced hyperactivity) are used. For Alzheimer's disease research, transgenic mouse models are employed. Brain penetration is confirmed by measuring drug levels in brain tissue.
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| ADME/Pharmacokinetics |
MEM-1003 has a molecular weight of approximately 400 g/mol. CAS number: 165187-25-7. It is a racemic formulation. Store as a powder at -20°C. Soluble in DMSO. The compound is brain-penetrant. Pharmacokinetic parameters such as oral bioavailability, plasma half-life, and brain penetration have been characterized in preclinical studies. For in vivo use, formulate in suitable vehicle.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available for MEM-1003. As a research compound, it is not intended for human use and has not undergone formal toxicological evaluation. Standard preclinical safety assessments for calcium channel blockers would include cardiovascular safety assessment (hypotension, bradycardia), hERG channel inhibition, and CNS side effect profiling. The compound is for research use only.
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| References | |
| Additional Infomation |
MEM-1003 is a research-grade L-type calcium channel blocker with brain penetration. It is not approved for clinical use. Also known as BAY-Z-4406. The compound is a dihydropyridine derivative. It has potential applications in bipolar disorder and Alzheimer's disease research. MEM-1003 is supplied as a powder with high purity and should be stored desiccated at -20°C.
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| Molecular Formula |
C22H25CLN2O5
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|---|---|
| Molecular Weight |
432.8973
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| Exact Mass |
432.145
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| CAS # |
165187-25-7
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| PubChem CID |
9802887
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
30
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| Complexity |
780
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C#N)C([H])=C([H])C([H])=C1C1([H])C(C(=O)OC([H])([H])C([H])([H])OC([H])([H])[H])=C(C([H])([H])[H])N([H])C(C([H])([H])[H])=C1C(=O)OC([H])(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
GTIKSQYSAKETQA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H25ClN2O5/c1-12(2)30-22(27)18-14(4)25-13(3)17(21(26)29-10-9-28-5)19(18)16-8-6-7-15(11-24)20(16)23/h6-8,12,19,25H,9-10H2,1-5H3
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| Chemical Name |
3-O-(2-methoxyethyl) 5-O-propan-2-yl 4-(2-chloro-3-cyanophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
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| Synonyms |
MEM1003; BAY-Z-4406; MEM-1003
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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 : ~125 mg/mL (~288.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.80 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 20.8 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: 2.08 mg/mL (4.80 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (4.80 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 | 2.3100 mL | 11.5500 mL | 23.1000 mL | |
| 5 mM | 0.4620 mL | 2.3100 mL | 4.6200 mL | |
| 10 mM | 0.2310 mL | 1.1550 mL | 2.3100 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.