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NNC 55-0396

In stock
Catalog No.
A3662
T-type calcium channel blocker
Grouped product items
SizePriceStock Qty
5mg
$168.00
In stock
10mg
$240.00
In stock

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Background

IC50: 6.8 μM for Cav3.1 T-type channel

NNC 55-0396 is a T-type calcium channel antagonist.

T-type calcium channel activity is reported to be a critical component of the spontaneous voltage oscillation of inferior olive neurons occurring at a frequency similar to that of essential tremor.

In vitro: NNC 55-0396 showed no effect against high voltage calcium channels at 100 μM, but inhibited T-type channels in HEK293 cells with a potency comparable to that of mibefradil (IC50 6.8 versus 10.1 μM) [1].

In vivo: NNC 55-0396 was better tolerated than mibefradil in the horizontalwire test. To assess for a potential interaction with harmaline in the inverted wire grid test, mice was given NNC 55-0396, followed by harmaline or vehicle. NNC 55-0396 ameliorated harmaline-induced test deficits. In the GABAA α1-null model, NNC 55-0396 at 12.5 mg/kg suppressed harmaline-induced tremor by half by 20–100 min, whereas mibefradil at the same dose did not significantly affect tremor. In contrast to mibefradil, NNC 55-0396 was well tolerated and suppresses tremor, and exerts less cytochrome P450 inhibition [1].

Clinical trial: N/A

Reference:
[1] Quesada A,Bui PH,Homanics GE,Hankinson O,Handforth A. Comparison of mibefradil and derivative NNC 55-0396 effects on behavior, cytochrome P450 activity, and tremor in mouse models of essential tremor. Eur J Pharmacol.2011 May 20;659(1):30-6.

Chemical Properties

Physical AppearanceWhite solid
StorageStore at -20°C
M.Wt564.56
Cas No.357400-13-6
FormulaC30H40Cl2FN3O2
SynonymsNNC 55-0396 dihydrochloride
SolubilitySoluble to 25 mM in sterile water
Chemical Name2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)(methyl)amino)ethyl)-6-fluoro-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl cyclopropanecarboxylate dihydrochloride
SDFDownload SDF
Canonical SMILESCC(C1C2=C(C=C(F)C=C2)CCC1(OC(C3CC3)=O)CCN(CCCC4=NC5=CC=CC=C5N4)C)C.Cl.Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

NNC 55-0396