ML218
Based on 2 publication(s) in Google Scholar
ML218 is a potent, selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier.
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- Purity: 99.49%
- CAS No.: 1346233-68-8
- 화학식: C19H26Cl2N2O
- 분자량:369.33
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ML218
MoreAll Calcium Channel Isoforms
More
Biological Activity
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T-type calcium channel |
In plasma protein binding studies (equilibrium dialysis), ML218 possesses good free fraction in both rat and human. Intrinsic clearance experiments in liver microsomes indicated that ML218 is highly cleared in rat (CLint = 115 mL/min/kg), but low to moderately cleared in human liver microsomes (CLint = 12.7 mL/min/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Free brain and plasma concentrations of ML218 increases in a dose proportional manner across the dose range (3 mg/kg: [plasma] = 98 nM, [brain] = 1.66 μM; 10 mg/kg: [plasma] = 282 nM, [brain] = 5.03 μM; 30 mg/kg: 1.2 μM, [brain] = 17.7 μM)[1].
Noncompartmental pharmacokinetic analysis indicates ML218 (1 mg/kg, IV) has a mean residence time (MRT) of nearly 7 h, a value which is consistent with its terminal half-life (t1/2 = 7 h)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (275-299 g) induced by haloperidol[1]
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Dosage:0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Oral administration; once
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Result:Reversed cataleptic behavior in rats induced by a 0.75 mg/kg dose of haloperidol.
Chemical Information
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CAS No. 1346233-68-8
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Appearance Solid
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분자량 369.33
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화학식 C19H26Cl2N2O
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Color White to off-white
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SMILES
O=C(NC[C@@H]1[C@@]2([H])CN(CCC(C)(C)C)C[C@@]12[H])C3=CC(Cl)=CC(Cl)=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Biomaterials
Electroactive membranes enhance in-situ alveolar ridge preservation via spatiotemporal electrical modulation of cell motility. [Abstract]2024 Dec 31:317:123077. PMID: 39756273 -
Mol Genet Genomics
CACNA1H restrains chemotherapy resistance in ovarian clear cell carcinoma cells by repressing autophagy. [Abstract]2024 Aug 6;299(1):77. PMID: 39105964
용액&용해도
DMSO : 125 mg/mL (338.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (273 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7076 mL | 13.5380 mL | 27.0761 mL | 67.6901 mL |
| 5 mM | 0.5415 mL | 2.7076 mL | 5.4152 mL | 13.5380 mL | |
| 10 mM | 0.2708 mL | 1.3538 mL | 2.7076 mL | 6.7690 mL | |
| 15 mM | 0.1805 mL | 0.9025 mL | 1.8051 mL | 4.5127 mL | |
| 20 mM | 0.1354 mL | 0.6769 mL | 1.3538 mL | 3.3845 mL | |
| 25 mM | 0.1083 mL | 0.5415 mL | 1.0830 mL | 2.7076 mL | |
| 30 mM | 0.0903 mL | 0.4513 mL | 0.9025 mL | 2.2563 mL | |
| 40 mM | 0.0677 mL | 0.3385 mL | 0.6769 mL | 1.6923 mL | |
| 50 mM | 0.0542 mL | 0.2708 mL | 0.5415 mL | 1.3538 mL | |
| 60 mM | 0.0451 mL | 0.2256 mL | 0.4513 mL | 1.1282 mL | |
| 80 mM | 0.0338 mL | 0.1692 mL | 0.3385 mL | 0.8461 mL | |
| 100 mM | 0.0271 mL | 0.1354 mL | 0.2708 mL | 0.6769 mL |
ML218 Related Classifications
HY-103309 Related Classifications
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