KY-226

製品コードS0136 バッチS013601

印刷

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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), this compound up to 10 μM has no effects on adipocyte differentiation. In human hepatoma-derived cells (HepG2), this chemical (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. This compound attenuates plasma glucose elevations in the oral glucose tolerance test. It also increases pIR and phosphorylated Akt in the liver and femoral muscle. In high-fat diet-induced obese mice, the oral administration of this chemical (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 KY-226 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

https://pubmed.ncbi.nlm.nih.gov/29731242/

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。

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。