A selective inhibitor of T-type calcium channels (IC50 = 6.8 μM); exhibits no activity against L-type calcium channels up to 100 μM; inhibits tremor in mice (20 mg/kg and 12.5 mg/kg in GABAA α1-null and harmaline-induced tremor models

NNC 55-0396 – 25 mg

Brand:
Cayman
CAS:
357400-13-6
Storage:
-20
UN-No:
Non-Hazardous - /

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.{34694} 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 (Item No. 15037).{34695} In arterial smooth muscle cells, NCC 55-0396 (IC50 = 80 nM) inhibits voltage-dependent K+ channels but does not affect their voltage sensitivity.{34696} 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.{34697}  

 

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Description

A selective inhibitor of T-type calcium channels (IC50 = 6.8 μM); exhibits no activity against L-type calcium channels up to 100 μM; inhibits tremor in mice (20 mg/kg and 12.5 mg/kg in GABAA α1-null and harmaline-induced tremor models, respectively); inhibits Kv channels (IC50 = 80 nM)

Formal name: cyclopropanecarboxylic acid, (1S,2S)-2-[2-[[3-(1H-benzimidazol-2-yl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenyl ester, dihydrochloride

Synonyms: 

Molecular weight: 564.6

CAS: 357400-13-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Transcription Factors|HIF-1α||Research Area|Cancer|Tumor Microenvironment||Research Area|Cardiovascular System|Vasculature|Smooth Muscle Cells||Research Area|Cell Biology|Cell Signaling|Calcium Mobilization||Research Area|Neuroscience

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