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ML 218 hydrochloride

MLS003431854, SMR002112449, VU0413807-1, VU0413807-2, VU0424199-1

A Selective Blocker of T-type Channels

Cat #: M-166
Alternative Name MLS003431854, SMR002112449, VU0413807-1, VU0413807-2, VU0424199-1
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 405.8
    Purity: >98%
    Form Lyophilized powder.
    Effective concentration 0.1-100 µM.
    Structure
    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.
    Molecular formula C19H26Cl2N2O●HCl.
    CAS No.: 1346233-68-8
    Activity ML 218 is a blocker of T-type Ca2+ channels (IC50 values are 270 and 310 nM for CaV3.3 and CaV3.2 respectively)1.
    References-Activity
    1. Xiang, Z. et al. (2011) ACS Chem. Neurosci. 2, 730.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs ML 218 hydrochloride inhibits T-type CaV channels heterologously expressed in Xenopus oocytes.
      Alomone Labs ML 218 hydrochloride inhibits T-type CaV channels heterologously expressed in Xenopus oocytes.
      A. Time course of CaV3.2 peak current amplitude, elicited by 100 ms voltage step from holding potential of -100 mV to -30 mV, delivered every 10 seconds. Application of 2 µM ML 218 hydrochloride (#M-166) inhibits the CaV3.2 current in a reversible manner (indicated by the horizontal bar). B. Representative current traces before and during application of 2 µM ML 218 hydrochloride as indicated.
    References - Scientific background
    1. Xiang, Z. et al. (2011) ACS Chem. Neurosci. 2, 730.
    2. Xie, X. et al. (2011) Probe Reports from the NIH Molecular Libraries Program.
    Scientific background T-Type Ca2+ channel inhibitors hold tremendous therapeutic potential for the treatment of pain, epilepsy, sleep disorders, essential tremor, and other neurological disorders1. ML 218 is a selective, potent inhibitor of T-type Ca2+ channels (IC50 values are 270 and 310 nM for CaV3.3 and CaV3.2 respectively in a patch EP assay). It has no activity on other members of the Ca2+ family of ion channels (L- and N-type Ca2+ channels) as well as multiple Na+ and K+ channels. ML 218 was found to be non-selective against hERG and many other ion channels. ML 218 possess excellent DMPK properties, acceptable in vivo rat PK, excellent brain levels and was efficacious in a haloperidol-induced catalepsy assay, a preclinical Parkinsonian model. ML 218 decreases burst activity in subthalamic nucleus (STN) neurons. Thus, ML 218 is a powerful new probe to study T-Type Ca2+ function both in vitro and in vivo2.
    Target T-type CaV channels
    Lyophilized Powder
    Last update: 02/01/2022

    ML 218 hydrochloride (#M-166) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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