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
- CAS No.
- 1256269-87-0
- Chemical Name:
- 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
- Synonyms
- SAK3 >=98% (HPLC);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;Spiro[2-cyclopentene-1,3'(2'H)-imidazo[1,2-a]pyridine]-3-carboxylic acid, 8'-methyl-2',4-dioxo-2-(1-piperidinyl)-, ethyl ester
- CBNumber:
- CB34902723
- Molecular Formula:
- C20H23N3O4
- Molecular Weight:
- 369.41
- MDL Number:
- MOL File:
- 1256269-87-0.mol
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 Properties
Boiling point | 539.3±60.0 °C(Predicted) |
---|---|
Density | 1.37±0.1 g/cm3(Predicted) |
storage temp. | Store at 4°C |
solubility | Soluble in DMSO |
pka | 3.36±0.20(Predicted) |
form | Solid |
color | White to off-white |
FDA UNII | YJ4M3A4ZH4 |
UNSPSC Code | 12352200 |
NACRES | NA.77 |
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 price
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 Chemical Properties,Uses,Production
Uses
SAK3 is a potent CaV3.1 and CaV3.3 activator. Enhances CaV3.1 and CaV3.3, but not CaV3.2 activity at concentrations of 0.01 - 10 M in neuro2A cells in vitro. Elevates ACh levels in hippocampus. Rescues impaired memory-related behaviors in OBX mice. Orally bioavailable.
Biological Activity
SAK3 is a potent and orally active spiroimidazopyridine derivative th at 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 na?ve 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).
in vivo
Acute SAK3 (0.5 mg/kg) oral administration promotes acetylcholine (ACh) release in hippocampal CA1 via T-VGCC stimulation via enhancing T-type Ca2+ channel[1].
Animal Model: | Animal Model:Cav3.1 knockout (KO) mice[1] |
Dosage: | 0.5 mg/kg |
Administration: | Administered p.o. |
Result: | Significantly increased ACh release in CA1, peaking at 20 min after oral administration. |
IC 50
T-type calcium channel
storage
Store at +4°C
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 Preparation Products And Raw materials
Raw materials
Preparation Products
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 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32376 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
HangZhou YuHao Chemical Technology Co., Ltd. | 0571-82693216 | info@yuhaochemical.com | China | 2028 | 58 |
Shanghai Hongye Biotechnology Co. Ltd | 400-9205774 | sales@glpbio.cn | China | 6777 | 58 |
BOC Sciences | -- | info@bocsci.com | USA | 0 | 65 |
Energy Chemical | 021-58432009 400-005-6266 | marketing1@energy-chemical.com | China | 44813 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24982 | 58 |
Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 5656 | 58 |
Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11973 | 58 |