An inhibitory gating modifier of SK channels (Kds = 0.42

NS 8593 (hydrochloride) – 25 mg

Brand:
Cayman
CAS:
875755-24-1
Storage:
-20
UN-No:
Non-Hazardous - /

NS 8593 is an inhibitory gating modifier of small conductance calcium-activated potassium (SK) channels (Kds = 0.42, 0.6, and 0.73 μM for SK1, SK2, and SK3, respectively, in the presence of calcium) that decreases the calcium sensitivity of SK channels.{53292} It is selective for SK channels over intermediate (IK) and large conductance (BK) potassium channels at 10 μM. NS 8593 induces relaxation of potassium- or acetylcholine chloride-precontracted isolated tracheal rings from wild-type mice (IC50s = 8.9 and 39.8 μM, respectively) or from mice in an ovalbumin-induced model of allergic asthma (IC50s = 16.4 and 32.2 μM, respectively).{53293} It inhibits aerosolized acetylcholine chloride-induced increases in respiratory system resistance in mice when administered as an aerosol at a dose of 500 μM. NS 8593 (5 mg/kg) decreases the duration of burst-pacing-induced atrial fibrillation in normotensive and spontaneously hypertensive rats.{53294}  

 

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Description

An inhibitory gating modifier of SK channels (Kds = 0.42, 0.6, and 0.73 μM for SK1, SK2, and SK3, respectively, in the presence of calcium); decreases the calcium sensitivity of SK channels; selective for SK channels over IK and BK potassium channels at 10 μM; induces relaxation of potassium- or acetylcholine chloride-precontracted isolated tracheal rings from wild-type mice (IC50s = 8.9 and 39.8 μM, respectively) or from mice in an ovalbumin-induced model of allergic asthma (IC50s = 16.4 and 32.2 μM, respectively); inhibits aerosolized acetylcholine chloride-induced increases in respiratory system resistance in mice when administered as an aerosol at 500 μM; decreases the duration of burst-pacing-induced atrial fibrillation in normotensive and spontaneously hypertensive rats at 5 mg/kg

Formal name: N-[(1R)-1,2,3,4-tetrahydro-1-naphthalenyl]-1H-benzimidazol-2-amine, monohydrochloride

Synonyms: 

Molecular weight: 299.8

CAS: 875755-24-1

Purity: ≥98%

Formulation: A solid

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