Biological Activity
Selective inhibitor of T-type calcium channels (IC50 values are 270 and 310 nM for Cav3.3 and Cav3.2 respectively in a patch EP assay). Decreases burst activity in STN neurons; reduces cataleptic behaviour in an in vivo rat model of Parkinson's disease. Displays no significant inhibition of L- or N-type calcium channels, Kir6 (KATP) or KV11.1 (hERG) potassium channels. Orally active.
Compound Libraries
ML 218 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 405.79 |
| Formula | C19H26Cl2N2O.HCl |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1346233-68-8 |
| PubChem ID | 2723792 |
| InChI Key | JIQFFACVQXXHMY-YDALLXLXSA-N |
| Smiles | CC(C)(C)CCN1C[C@@]2([H])[C@@]([C@@H]2CNC(C3=CC(Cl)=CC(Cl)=C3)=O)([H])C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 36.93 | 100 | |
| ethanol | 36.93 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 405.79. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.46 mL | 12.32 mL | 24.64 mL |
| 5 mM | 0.49 mL | 2.46 mL | 4.93 mL |
| 10 mM | 0.25 mL | 1.23 mL | 2.46 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
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References
References are publications that support the products' biological activity.
Xiang et al (2011) The discovery and characterization of ML218: A novel, centrally active T-type calcium channel inhibitor with robust effects in STN neurons and in a rodent model of Parkinson's disease. ACS Chem.Neurosci. 2 730 PMID: 22368764
Galvan et al (2016) Lack of antiparkinsonian effects of systemic injections of the specific T-type calcium channel blocker ML218 in MPTP-treated monkeys. ACS Chem.Neurosci 7 1543 PMID: 27596273
Keywords: ML 218 hydrochloride, supplier, ML218, HCl, CID45115620, T-type, calcium, channels, CAV3.1, CAV3.2, CAV3.3, inhibitors, inhibits, selective, Voltage-gated, Calcium, Channels, Voltage-gated, Calcium, Channels, Tocris Bioscience
