SAK3

SAK3

Biochem/physiol Actions

SAK3 is a potent and orally active spiroimidazopyridine derivative that enhances Cav3.1 and Cav3.3, but not Cav3.2, T-type voltage-gated Ca2+ channel (T-VGCC) activity (~20% peak current increase with 0.1 nM SAK3 by whole-cell patch-clamp using human Cav3.1 or Cav3.3 transfected neuro2A; no effect up to 10 nM using Cav3.2 transfectant). Acute SAK3 oral administration (0.5 mg/kg) significantly enhances hippocampal CA1 region acetylcholine (ACh) release in naïve mice, as well as increases hippocampal ACh levels and improves memory deficits among olfactory-bulbectomized (OBX) mice. Daily SAK3 oral administration 24 hrs following hypothyroidism induction by methimazole (MMI) is efficacious against MMI-induced medial septum (MS) cholinergic neurons loss (0.5-1 mg/kg/day) and cognitive deficits (1 mg/kg/day).

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575734 SAK3 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear
£461.04 (exc VAT) per 25MG
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3575735 SAK3 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear
£121.32 (exc VAT) per 5MG
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