SML2039

SAK3

≥98% (HPLC)

• Synonym(e): 8′-Methyl-2′,4-dioxo-2-(1-piperidinyl)-spiro[2-cyclopentene-1,3′(2′H)-imidazo[1,2-a]pyridine]-3-carboxylic acid ethyl ester, Ethyl 8′-methyl-2′,4-dioxo-2-(piperidin-1-yl)-2′H-spiro[cyclopent[2]ene-1,3′-imidazo[1,2-a]pyridine]-3-carboxylate
• Empirische Formel (Hill-System): C₂₀H₂₃N₃O₄
• CAS-Nummer: 1256269-87-0
• Molekulargewicht: 369.41
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: O=C(OCC)C1=C(C2(CC1=O)N3C=CC=C(C3=NC2=O)C)N4CCCCC4
• InChI key: WZHBYTVHUFURPY-UHFFFAOYSA-N

Beschreibung

Biochem/physiol Actions

Potent and orally active Cav3.1 & Cav3.3 T-type voltage-gated Ca2+ channel (T-VGCC) enhancer with in vivo cognitive deficits-improving efficacy.

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).

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable