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Submit ReviewML 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.
ML 218 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 405.79 |
公式 | C19H26Cl2N2O.HCl |
储存 | Store at +4°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 36.93 | 100 | |
ethanol | 36.93 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 ML 218 hydrochloride 的部分引用包括:
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
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
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
Nisha et al (2015) T-type calcium channels contribute to calcium disturbances in brain during hyponatremia. Exp Neurol 273 105-13 PMID: 26257025
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
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
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