ML352 |
Catalog No.GC12507
One-Click Copy Product Info
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Non-competitive inhibitor of the presynaptic choline transporter
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1649450-12-3
Sample solution is provided at 25 µL, 10mM.
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The neurotransmitter acetylcholine (ACh) plays a critical role in autonomic function, motor control, attention, learning, and memory, and reward. The high-affinity choline transporter (CHT) is the ratelimiting determinant of ACh synthesis, yet the transporter remains a largely undeveloped target for the detection and manipulation of synaptic cholinergic signaling. ML352 is a novel, noncompetitive inhibitor of the presynaptic choline transporter.
In vitro: At concentrations fully antagonized CHT in transfected cells and nerve terminal preparations, ML352 exhibited no inhibition of acetylcholinesterase or cholineacetyltransferase and also lacked activity at dopamine, serotonin, and norepinephrine transporters, as well as many receptors and ion channels. ML352 exhibited noncompetitive choline uptake inhibition in intact cells and reduced the apparent density of hemicholinium-3 binding sites in membrane assays, indicating allosteric transporter interactions [1].
In vivo: DMPK studies revealed a high intravenous plasma clearance, a combination of the oral bioavailability and total brain concentrations indicate ML352 to be a suitable probe for studies of altered in vivo ACh signaling and behavioral effects in rodents [2].
Clinical trial: Up to now, ML352 is still in the preclinical development stage.
Reference:
[1] Ennis EA, Wright J, Retzlaff CL, McManus OB, Lin Z, Huang X, Wu M, Li M, Daniels JS, Lindsley CW, Hopkins CR, Blakely RD. Identification and characterization of ML352: a novel, noncompetitive inhibitor of the presynaptic choline transporter. ACS Chem Neurosci. 2015 Mar 18;6(3):417-27.
[2] Elizabeth Ennis Miss, Jane Wright, James Tarr, Charles Locuson, Corey Hopkins, J Daniels, Craig Lindsley and Randy Blakely. A Novel Approach to Cholinergic Signaling Modulation: Development and Characterization of ML352, a Novel, Noncompetitive Inhibitor of the Presynaptic Choline Transporter. The FASEB Journal vol. 29 no. 1 Supplement 932.6
| Cas No. | 1649450-12-3 | SDF | |
| Chemical Name | (Z)-N-((3-isopropylisoxazol-5-yl)methyl)-4-methoxy-3-((1-methylpiperidin-4-yl)oxy)benzimidic acid | ||
| Canonical SMILES | CC(C1=NOC(C/N=C(O)/C2=CC(OC(CC3)CCN3C)=C(OC)C=C2)=C1)C | ||
| Formula | C21H29N3O4 | M.Wt | 387.47 |
| Solubility | 5mg/mL in ethanol, 20mg/mL in DMSO or DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5808 mL | 12.9042 mL | 25.8084 mL |
| 5 mM | 516.2 μL | 2.5808 mL | 5.1617 mL |
| 10 mM | 258.1 μL | 1.2904 mL | 2.5808 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A jelly
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)