KC 12291 hydrochloride

Product details

• Chemical name: 3,4-Dimethoxy-N-methyl-N-[3-[(5-phenyl-1,2,4-thiadiazol-3-yl)oxy]propyl]benzeneethanamine hydrochloride.
• CAS number: 181936-98-1
• Molecular formula: C22H27N3O3S•HCl.
• Purity: >97%
• Concentration: 0.5 - 100 μM.
• Form: Lyophilized Powder
• Solubility: DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
• Reconstitution: DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
• Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
• Target: NaV channels
• Source: Synthetic
• Activity: Orally active voltage-gated Na+ (NaV) channel blocker1-2 with cardioprotective properties2-4. Inhibits sustained Na+ currents (INaL) with IC50 of 9.6 μM and prevents diastolic contracture in isolated atrial myocytes (IC50 of about 0.7 μM)5.

Scientific background

The pathophysiological importance of Na+ overload is highlighted by the fact that a variety of drugs reducing Na+ influx proved to be cardioprotective, both at the intact organ and cellular level. In addition, a correlation between the degree of Na+ channel blockade and functional recovery from myocardial infarction is established1.KC 12291 is an orally active atypical voltage-gated sodium channel blocker with cardioprotective properties2-4. It effectively blocks cardiac voltage-gated sodium channels, involving inhibition of the peak Na+ current and thus delays Na+ overload during ischemia by enhancing the inexcitability of the heart4-5.KC 12291 abolishes diastolic contracture in isolated myocytes obtained from guinea-pig atria, with IC50 values of 0.55 and 0.79 μM respectively, and the IC50 for KC 12291 inhibition of the sustained component of Na+ current, INaL, is 9.6 μM6.KC 12291 exerts a potent bradycardic effect in the rat7.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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