Tofogliflozin(CSG 452)

製品コードS8558 バッチS855801

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₂H₂₆O₆.H₂O

分子量

404.45

CAS No.

1201913-82-7

Solubility (25°C)*

体外

DMSO

84 mg/mL (207.68 mM)

Ethanol

84 mg/mL (207.68 mM)

Water

4 mg/mL (9.88 mM)

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	Tofogliflozin (CSG 452)は、hSGLT2およびHsglt1に対してそれぞれ2.9 nMおよび8444 nMのIC50値を有する新規のナトリウム-グルコース共輸送体2(SGLT2)阻害剤です。
in vitro	Tofogliflozin (CSG 452) is a potent and highly selective SGLT2 inhibitor, with 2900-fold greater selectivity for SGLT2 over SGLT1. It dose-dependently inhibited glucose entry into tubular cells, suppressed high glucose-induced ROS generation, MCP-1 gene induction, and apoptosis in tubular cells. An antioxidant NAC mimicked the effects of this compound on high glucose-exposed tubular cells.
in vivo	Tofogliflozin (CSG 452), when administered as a single oral dose, lowers blood glucose levels in Zucker diabetic rats by increasing renal glucose clearance. A four-week treatment with this compound improves glucose tolerance in db/db mice. It also reduces urine volume compared with the untreated control group at 8 weeks of treatment. Compared with untreated db/db mice, treatment increases renal glucose clearance levels, whereas losartan has no effect on this parameter. It reduces the threshold of glucose reabsorption in db/db mice, increases UGE, and subsequently lowers PG. Additionally, treatment significantly and dose-dependently elevates total beta-cell mass, suggesting prevention of beta-cell loss. Tofogliflozin suppresses plasma glucose and glycated Hb while preserving pancreatic beta-cell mass and plasma insulin levels.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Tubular cells
	濃度	3 nM or 30 nM
	反応時間	24 h
	実験の流れ	Tubular cells are treated with or without 3 nM or 30 nM tofogliflozin (CSG 452) under serum-free BM containing 10 μg/ml transferrin and GA-1 000 for 24 h at 37 °C. After washing with PBS, the cells are incubated with Hanks’ balanced salt solution (HBSS) containing 100 μM of 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino]-2-deoxy-d-glucose (2-NBDG), a fluorescent derivative of glucose, in the absence of this compound for 15 min. Culture medium is removed and replaced with HBSS, and fluorescence intensity in the cells is analyzed in an ARVO fluorescent plate reader.
動物実験	動物モデル	db/db mice
	投薬量	0.005 or 0.015%
	投与方法	oral

参考

http://pubs.acs.org/doi/abs/10.1021/jm300884k
https://pubmed.ncbi.nlm.nih.gov/23751087/
https://pubmed.ncbi.nlm.nih.gov/26158396/

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。