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SML0385

Sigma-Aldrich

ML218

≥98% (HPLC)

Sinonimo/i:

3,5-Dichloro-N-[[(1α,5α,6-exo,6α)-3-(3,3-dimethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]methyl]benzamide, CID 45115620, VU0413807, VU0424199-1

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About This Item

Formula empirica (notazione di Hill):
C19H26Cl2N2O
Numero CAS:
1346233-68-8
Peso molecolare:
369.33
Codice UNSPSC:
12352200
ID PubChem:
329825385
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥98% (HPLC)

Stato

powder

Colore

white to beige

Solubilità

DMSO: 10 mg/mL (clear solution)

Temperatura di conservazione

2-8°C

Stringa SMILE

CC(C)(C)CCN1C[C@H]2C(CNC(=O)c3cc(Cl)cc(Cl)c3)[C@H]2C1

InChI

1S/C19H26Cl2N2O/c1-19(2,3)4-5-23-10-16-15(17(16)11-23)9-22-18(24)12-6-13(20)8-14(21)7-12/h6-8,15-17H,4-5,9-11H2,1-3H3,(H,22,24)/t15-,16-,17+
GSJIGYLGKSBYBC-OSYLJGHBSA-N

Applicazioni

ML218 has been used as a:
  • T-type channel blocker to test its effect on the nociceptive behavior associated with homocysteinemia rats
  • T-type voltage-sensitive calcium channel (VSCC) inhibitor in osteoblasts
  • T-type calcium channel blocker to test its effect on the viability of neural progenitor cells

Azioni biochim/fisiol

ML218 (CID 45115620) is a potent and selective T-Type (Cav3.1, Cav3.2, Cav3.3) calcium channel inhibitor (Cav3.2, IC50 = 150 nM in Ca2+ flux; Cav3.2 IC50 = 310 nM and Cav3.3 IC50 = 270 nM with good Drug metabolism/Pharmacokinetics. In a panel of 68 GPCRs, ion channels and transporters, ML218 was found to bind significantly only two other targets (sodium channel site 2 and sigma 1) and had no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. It showed robust inhibition of calcium current in STN neurons and was orally active in a rodent model of Parkinson′s Disease.

Caratteristiche e vantaggi

This compound is featured on the Calcium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

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Certificati d'analisi (COA)

Lot/Batch Number
072M4612V

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Brittany D Spitznagel et al.
ACS chemical neuroscience, 11(21), 3658-3671 (2020-11-05)
Malignant migrating partial seizures of infancy is a rare, devastating form of epilepsy most commonly associated with gain-of-function mutations in the potassium channel, Slack. Not only is this condition almost completely pharmacoresistant, there are not even selective drug-like tools available
Retsu Mitsui et al.
Pflugers Archiv : European journal of physiology, 468(2), 279-291 (2015-11-05)
Postcapillary venules (PCVs) play a critical role in regulating capillary hydrostatic pressure, but their contractile mechanisms are not well understood. We examined the properties of spontaneous vasomotion and corresponding Ca(2+) transients in gastric PCV. In the rat gastric submucosa, changes
Andreas Feigenspan et al.
Experimental eye research, 195, 108028-108028 (2020-04-12)
Expression patterns of voltage-gated ion channels determine the spatio-temporal dynamics of ion currents that supply excitable neurons in developing tissue with proper electrophysiological properties. The purpose of the study was to identify fast cationic inward currents in mouse retinal horizontal
Kaori Sato-Numata et al.
The journal of physiological sciences : JPS, 70(1), 49-49 (2020-10-17)
Arginine vasopressin (AVP) neurons play essential roles in sensing the change in systemic osmolarity and regulating AVP release from their neuronal terminals to maintain the plasma osmolarity. AVP exocytosis depends on the Ca2+ entry via voltage-gated Ca2+ channels (VGCCs) in
Nicholas Mikolajewicz et al.
eLife, 7 (2018-10-17)
Bone cells sense and actively adapt to physical perturbations to prevent critical damage. ATP release is among the earliest cellular responses to mechanical stimulation. Mechanical stimulation of a single murine osteoblast led to the release of 70 ± 24 amole
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