| Identification | Back Directory | [Name]
NNC 55-0396 dihydrochloride | [CAS]
357400-13-6 | [Synonyms]
NNC 55-0396 DIHYDROCHLORIDE
(1S,2S)-2-[2-[[3-(1H-BENZIMIDAZOL-2-YL)PROPYL]METHYLAMINO]ETHYL]-6-FLUORO-1,2,3,4-TETRAHYDRO-1-(1-METHYLETHYL)-2-NAPHTHALENYL CYCLOPROPANECARBOXYLATE DIHYDROCHLORIDE | [Molecular Formula]
C30H40Cl2FN3O2 | [MDL Number]
MFCD08703107 | [MOL File]
357400-13-6.mol | [Molecular Weight]
564.562 |
| Chemical Properties | Back Directory | [Melting point ]
174 - 179°C | [storage temp. ]
Desiccate at RT | [solubility ]
DMSO (Slightly), Water (Slightly) | [form ]
Solid | [color ]
White to Off-White | [Water Solubility ]
Soluble to 25 mM in water | [Stability:]
Hygroscopic |
| Hazard Information | Back Directory | [Description]
NNC 55-0396 is a selective inhibitor of T-type calcium channels that blocks Cav3.1 in stably expressing HEK293 cells (IC50 = 6.8 μM) with no discernible effect on high voltage-activated (L-type) channels in INS-1 cells up to a concentration of 100 μM. NNC 55-0396 suppresses tremor in two murine models, the GABAA α1-null (20 mg/kg) and harmaline-induced (12.5 mg/kg) tremor models, and was better tolerated than mibefradil . In arterial smooth muscle cells, NCC 55-0396 (IC50 = 80 nM) inhibits voltage-dependent K+ channels but does not affect their voltage sensitivity. NNC 55-0396 (1-5 μM) also suppresses angiogenesis in vitro by inhibiting hypoxia-inducible factor-1α activity, and it slows tumor growth of flank xenografts of U87MG cells in mice when administered at 20 mg/kg. | [Uses]
NNC 55-0396 is a calcium channel protein inhibitor. | [Definition]
ChEBI: NNC 55-0396 dihydrochloride is t-type calcium channel blocker It has a role as a calcium channel blocker. | [Biological Activity]
Highly selective T-type calcium channel blocker. Displays IC 50 values of 6.8 and > 100 μ M for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells. | [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]. | [IC 50]
6.8 μm for cav3.1 t-type channel | [storage]
Desiccate at RT | [References]
[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. |
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