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Submit ReviewML 218 hydrochloride
Description: CaV3.x blocker
Chemical Name: 3,5-Dichloro-N-[[(1α,5α,6-exo,6α)-3-(3,3-dimethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]methyl]-benzamide hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for ML 218 hydrochloride
ML 218 hydrochloride is a 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. ML 218 hydrochloride inhibits oral cancer cell proliferation. Orally active.
Compound Libraries for ML 218 hydrochloride
ML 218 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for ML 218 hydrochloride
| M. Wt | 405.79 |
| Formula | C19H26Cl2N2O.HCl |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 2319922-08-0 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for ML 218 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 36.93 | 100 | |
| ethanol | 36.93 | 100 |
Preparing Stock Solutions for ML 218 hydrochloride
The following data is based on the product molecular weight 405.79. Batch specific molecular weights may vary from batch to batch due to the degree 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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Product Datasheets for ML 218 hydrochloride
References for ML 218 hydrochloride
References are publications that support the biological activity of the product.
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
Chakraborty et al (2021) ML218 HCl is more efficient than capsaicin in inhibiting bacterial antigen-induced Cal 27 oral cancer cell proliferation. Int.J.Mol.Sci. 22 12559 PMID: 34830441
If you know of a relevant reference for ML 218 hydrochloride, please let us know.
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Keywords: ML 218 hydrochloride, ML 218 hydrochloride supplier, ML218, HCl, CID45115620, T-type, calcium, channels, CAV3.1, CAV3.2, CAV3.3, inhibitors, inhibits, selective, Cav3.x, Channels, 4507, Tocris Bioscience
6 Citations for ML 218 hydrochloride
Citations are publications that use Tocris products. Selected citations for ML 218 hydrochloride include:
Pascual-Caro et al (2018) STIM1 deficiency is linked to Alzheimer's disease and triggers cell death in SH-SY5Y cells by upregulation of L-type voltage-operated Ca2+ entry. J Mol Med (Berl) 96 1061 PMID: 30088035
Chakraborty et al (2021) ML218 HCl is more efficient than capsaicin in inhibiting bacterial antigen-induced Cal 27 oral cancer cell proliferation. Int.J.Mol.Sci. 22 12559 PMID: 34830441
Artem M et al (2021) Role of L-Type Voltage-Gated Calcium Channels in Epileptiform Activity of Neurons. Int J Mol Sci 22 PMID: 34638683
Nisha et al (2015) T-type calcium channels contribute to calcium disturbances in brain during hyponatremia. Exp Neurol 273 105-13 PMID: 26257025
Li et al (2017) MECHANISMS UNDERLYING ACTION OF XINMAILONG INJECTION, A TRADITIONAL CHINESE MEDICINE IN CARDIAC FUNCTION IMPROVEMENT. Afr J Tradit Complement Altern Med 14 241 PMID: 28573241
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
Do you know of a great paper that uses ML 218 hydrochloride from Tocris? Please let us know.
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