Overview
Alternative Name MLS003431854, SMR002112449, VU0413807-1, VU0413807-2, VU0424199-1
Lyophilized Powder yes
Source Synthetic
MW: 369.3
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.
Molecular formula C19H26Cl2N2O.
CAS No.: 1346233-68-8
PubChem CID 45115620
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
- 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 25 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 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 (#M-165) 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 as indicated.
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 effect 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
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
Citations
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