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Merck

N2538

Sigma-Aldrich

NS8593 -hydrochlorid

≥98% (HPLC), powder

Synonym(e):

: N-[(1R)-1,2,3,4-tetrahydro-1-naphthalenyl]-1H-Benzimidazol-2-amine hydrochloride

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About This Item

Empirische Formel (Hill-System):
C17H17N3 · HCl
CAS-Nummer:
Molekulargewicht:
299.80
UNSPSC-Code:
12352200
PubChem Substanz-ID:
NACRES:
NA.77

Assay

≥98% (HPLC)

Form

powder

Optische Aktivität

[α]/D +54 to +62°, c = 0.5 in methanol

Löslichkeit

DMSO: >10 mg/mL
H2O: insoluble

Lagertemp.

2-8°C

SMILES String

Cl[H].C1C[C@@H](Nc2nc3ccccc3[nH]2)c4ccccc4C1

InChI

1S/C17H17N3.ClH/c1-2-8-13-12(6-1)7-5-11-14(13)18-17-19-15-9-3-4-10-16(15)20-17;/h1-4,6,8-10,14H,5,7,11H2,(H2,18,19,20);1H/t14-;/m1./s1

InChIKey

VWEKCDTXUUPBNA-PFEQFJNWSA-N

Anwendung

NS8593 hydrochloride has been used to study its effect on the growth of MDA-MB-231 cells (M.D. Anderson and metastasis breast cancer cells).

Biochem./physiol. Wirkung

NS8593 hydrochloride inhibits small conductance calcium-activated potassium (SKCa) channels.
The compound (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphtylamine (NS8593) reversibly inhibited recombinant SK3-mediated currents (human and rat SK3) with potencies around 100 nM. NS8593 did not inhibit 125I-apamin binding. NS8593 decreased the calcium sensitivity by shifting the activation curve for Ca2+ to the right, only slightly affecting the maximal Ca2+-activated SK current. NS8593 inhibited all the SK1-3 subtypes Ca2+-dependently (Kd = 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca2+. NS8593 did not affect the calcium-activated potassium channels of intermediate and large conductance (hIK and hBK channels, respectively). NS8593-mediated inhibition was prevented in the presence of a high concentration of the positive modulator NS309.

Leistungsmerkmale und Vorteile

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

H-Sätze

Gefahreneinstufungen

Aquatic Chronic 4

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Persönliche Schutzausrüstung

Eyeshields, Gloves, type N95 (US)


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Die Dokumentenbibliothek aufrufen

Knockdown of the small conductance Ca2+-activated K+ channels is potently cytotoxic in breast cancer cell lines
Abdulkareem ZA, et al.
British Journal of Pharmacology, 173(1), 177-190 (2016)
Michiko Tashiro et al.
The journal of physiological sciences : JPS, 69(1), 97-102 (2018-06-18)
To examine whether TRPM7, a member of the melastatin family of transient receptor potential channels, is a physiological pathway for Mg2+ entry in mammalian cells, we studied the effect of TRPM7 regulators on cytoplasmic free Mg2+ concentration ([Mg2+]i) of rat
Francesca Luongo et al.
Nutrients, 10(6) (2018-06-19)
Intestinal magnesium (Mg) uptake is essential for systemic Mg homeostasis. Colon cells express the two highly homologous transient receptor potential melastatin type (TRPM) 6 and 7 Mg2+ channels, but their precise function and the consequences of their mutual interaction are
Alayna Mellott et al.
Pflugers Archiv : European journal of physiology, 472(11), 1589-1606 (2020-09-24)
TRPM7 is a cation channel-protein kinase highly expressed in T lymphocytes and other immune cells. It has been proposed to constitute a cellular entry pathway for Mg2+ and divalent metal cations such as Ca2+, Zn2+, Cd2+, Mn2+, and Ni2+. TRPM7
Goli Ardestani et al.
Cell calcium, 87, 102181-102181 (2020-02-26)
Prior to maturation, mouse oocytes are arrested at the germinal vesicle (GV) stage during which they experience constitutive calcium (Ca2+) influx and spontaneous Ca2+ oscillations. The oscillations cease during maturation but Ca2+ influx continues, as the oocytes' internal stores attain

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