KY-226

製品コードS0136 バッチS013601

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₇H₃₁NO₃S₂
	分子量	481.67	CAS No.	1621673-53-7
Solubility (25°C)*	体外	DMSO	96 mg/mL (199.3 mM)
		Ethanol	1.5 mg/mL (3.11 mM)
		Water	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	KY-226 is a potent, selective, orally active and allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 μM for human PTP1B activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively.
in vitro	KY-226 inhibits human PTP1B activity, but does not exhibit peroxisome proliferator-activated receptor γ (PPARγ) agonist activity. In rodent preadipocytes (3T3-L1), KY-226 up to 10 μM has no effects on adipocyte differentiation. In human hepatoma-derived cells (HepG2), KY-226 (0.3-10 μM) increases the phosphorylated insulin receptor (pIR) produced by insulin.^[1]
in vivo	In db/db mice, the oral administration of KY-226 (10 and 30 mg/kg/day, 4 weeks) significantly reduces plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain. KY-226 attenuates plasma glucose elevations in the oral glucose tolerance test. KY-226 also increases pIR and phosphorylated Akt in the liver and femoral muscle. In high-fat diet-induced obese mice, the oral administration of KY-226 (30 and 60 mg/kg/day, 4 weeks) decreases body weight gain, food consumption, and fat volume gain with increases in phosphorylated STAT3 in the hypothalamus.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	3T3-L1, HepG2
	濃度	0.1-10 μM
	反応時間	1 h
	実験の流れ	Cells with or without the overexpression of PTP1B are seeded at a density of 1 x 10 cells/well on 6-well plates and cultured for 24 h and then for 6 h in serumfree DMEM. Cells are cultured in the presence or absence of KY226 for 1 h, followed by an incubation with insulin for 10 min.Cells are washed and then used for various assays.
動物実験	動物モデル	db/db mice, high fat diet (HFD)-fed mice
	投薬量	10mg/kg, 30 mg/kg, 60 mg/kg
	投与方法	p.o.

参考

[1] Yuma Ito, et al. J Pharmacol Sci. 2018 May;137(1):38-46.

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：

Enhanced IFN Sensing by Aggressive Chronic Lymphocytic Leukemia Cells [ J Immunol, 2022, 209(9):1662-1673]	PubMed: 36104109

Enhanced IFN Sensing by Aggressive Chronic Lymphocytic Leukemia Cells [ J Immunol, 2022, 209(9):1662-1673]

PubMed: 36104109

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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