KGA-2727

製品コードS8938 バッチS893801

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₆H₄₀N₄O₈
	分子量	536.62	CAS No.	666842-36-0
Solubility (25°C)*	体外	DMSO	100 mg/mL (186.35 mM)
		Water	100 mg/mL (186.35 mM)
		Ethanol	45 mg/mL (83.85 mM)
* <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	KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models.
in vitro	KGA-2727 inhibits SGLT1 potently and highly selectively in an in vitro assay using cells transiently expressing recombinant SGLTs.^[1].
in vivo	In a small intestine closed loop absorption test with normal rats, KGA-2727 inhibits the absorption of glucose but not that of fructose. In the oral glucose tolerance test with streptozotocininduced diabetic rats, KGA-2727 attenuats the elevation of plasma glucose after glucose loading, indicating that KGA-2727 improves postprandial hyperglycemia. In Zucker diabetic fatty (ZDF) rats, chronic treatments with KGA-2727 reduces the levels of plasma glucose and glycated hemoglobin. Furthermore, KGA-2727 preserves glucose-stimulated insulin secretion and reduces urinary glucose excretion with improved morphological changes of pancreatic islets and renal distal tubules in ZDF rats. In addition, the chronic treatment with KGA-2727 increases the level of glucagon-like peptide-1 in the portal vein.^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	COS-7 cells
	濃度	0-1 μM, 0-100 μM
	反応時間	--
	実験の流れ	For the AMG uptake experiment, COS-7 cells are seeded into a 96-well collagen-coated culture plate at a density of 5 × 10⁴ cells/well in Dulbecco’s modified Eagle’s medium containing 10% fetal bovine serum. After 4 h, each plasmid is transfected into COS-7 cells using Lipofectamine 2000 and the cells are used 2 days after transfection. In this experiment, AMG uptake at 0.3 or 1 mM is measured in the presence of various concentrations of KGA-2727 to calculate Ki values.
動物実験	動物モデル	Male Wistar, Zucker diabetic fatty (ZDF) fa/fa (ZDF/Gmi Crl-fa/fa), and ZDF-lean (ZDF/Gmi Crl-lean) rats
	投薬量	10 mg/kg, 30 mg/kg, 100 mg/kg
	投与方法	Oral gavage

参考

[1] Shibazaki T, et al. J Pharmacol Exp Ther. 2012 Aug;342(2):288-96.

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。