Gliquidone

製品コードS3151 バッチS315102

化学情報

	Synonyms	Glurenorm,AR-DF 26	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₇H₃₃N₃O₆S
	分子量	527.63	CAS No.	33342-05-1
Solubility (25°C)*	体外	DMSO	100 mg/mL (189.52 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Gliquidone (Glurenorm,AR-DF 26) is an ATP-sensitive K⁺ channel antagonist with IC50 of 27.2 nM.
in vivo	Gliquidone (0.1–1.0 μg per mouse i.c.v.) prevents antinociception produced by amitriptyline and clomipramine in a dose-dependent manner in male swiss albino mice. ^[2] Gliquidone (0.06–16 μg per mouse, i.c.v.) antagonizes the antinociception induced by buprenorphine, morphine and methadone. ^[3] Gliquidone (6 μg per mouse, i.c.v.) prevents the antinociception induced by clonidine (0.125 mg/kg, s.c.) and guanabenz (0.30 mg/kg, s.c.), while a lower dose of gliquidone (3 μg per mouse, i.c.v.) is ineffective. ^[4] Glurenorm (10 mg/kg) given to the diabetic rats produces significant reductions in blood glucose, nonenzymatic glycosylation, and total protein in the lenses, and significantly increases in glutathione levels in the lenses. ^[5]

製品説明

Gliquidone (Glurenorm,AR-DF 26) is an ATP-sensitive K⁺ channel antagonist with IC50 of 27.2 nM.

in vivo

Gliquidone (0.1–1.0 μg per mouse i.c.v.) prevents antinociception produced by amitriptyline and clomipramine in a dose-dependent manner in male swiss albino mice. ^[2] Gliquidone (0.06–16 μg per mouse, i.c.v.) antagonizes the antinociception induced by buprenorphine, morphine and methadone. ^[3] Gliquidone (6 μg per mouse, i.c.v.) prevents the antinociception induced by clonidine (0.125 mg/kg, s.c.) and guanabenz (0.30 mg/kg, s.c.), while a lower dose of gliquidone (3 μg per mouse, i.c.v.) is ineffective. ^[4] Glurenorm (10 mg/kg) given to the diabetic rats produces significant reductions in blood glucose, nonenzymatic glycosylation, and total protein in the lenses, and significantly increases in glutathione levels in the lenses. ^[5]

プロトコル(参考用のみ)

キナーゼアッセイ	Binding assay
キナーゼアッセイ	[³H]Glibenclamide binding to cortex membranes is measured at 25 °C following an incubation period of 60 min. Binding assays are carried out by adding 200 μL of the membrane suspension to assay tubes containing 50 μL [³H]Glibenclamide (specific activity 52.7 Ci/mmol, 0.5 nM final concentration) and 50 μL Gliquidone in 50 mM Tris-HC1 buffer pH 7.4. Nonspecific binding is measured using 0.1 μM unlabeled glibenclamide. Assays are carried out in triplicate. Incubations are stopped by rapid filtration through Whatman GF/B filters under vacuum. The filters are immediately washed 3 times with 4 mL of ice-cold incubation buffer and their [³H]Glibenclamide content is counted with a iquid scintillation counter after addition of 10 mL of scintillation fluid. Equilibrium competitive inhibition experiments are carried out using the above assay conditions in the presence or absence of 10 different concentrations of Gliquidone. The concentration of Gliquidone that inhibits specific binding by 50% (IC50 value) is determined using ALLFIT or Ligand programs.

参考

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The Anti-diabetic Drug Gliquidone Modulates Lipopolysaccharide-Mediated Microglial Neuroinflammatory Responses by Inhibiting the NLRP3 Inflammasome [ Front Aging Neurosci, 2021, 13:754123]	PubMed: 34776934
Rescue of HSP70 in Spinal Neurons Alleviates Opioids-Induced Hyperalgesia via the Suppression of Endoplasmic Reticulum Stress in Rodents [ Front Cell Dev Biol, 2020, 8:269]	PubMed: 32500072
Validation of an LC-MS/MS method for analysis of anti-diabetic drugs in botanical dietary supplements labeled for blood sugar management [Ma J, et al. Drug Test Anal, 2018, 10(3):609-617]	PubMed: 28758363

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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