SML2039
SAK3
≥98% (HPLC)
동의어(들):
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
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C20H23N3O4
CAS Number:
Molecular Weight:
369.41
UNSPSC 코드:
12352200
NACRES:
NA.77
추천 제품
분석
≥98% (HPLC)
양식
powder
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
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
생화학적/생리학적 작용
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).
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
가장 최신 버전 중 하나를 선택하세요:
Husain Noreen et al.
Neurochemistry international, 108, 91-99 (2017-03-11)
Methimazole (MMI) is a first-line therapy used to manage hyperthyroidism and Graves' disease. Despite its therapeutic benefit, chronic MMI administration can lead to hypothyroidism and perturb brain homeostasis in patients, resulting in neuropsychiatric disorders such as depression and cognitive dysfunction.
Yasushi Yabuki et al.
Neuropharmacology, 117, 1-13 (2017-01-18)
T-type voltage-gated Ca
Udaiyappan Janakiraman et al.
Neurobiology of disease, 143, 105006-105006 (2020-07-06)
T-type calcium channels, in the central nervous system, are involved in the pathogenesis of many neurodegenerative diseases, including TAF1 intellectual disability syndrome (TAF1 ID syndrome). Here, we evaluated the efficacy of a novel T-type Ca2+ channel enhancer, SAK3 (ethyl 8'-methyl-2'
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