Sotagliflozin

製品コードS8103 バッチS810302

印刷

化学情報

Chemical Structure Synonyms LP-802034, LX4211 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H25ClO5S
分子量 424.94 CAS No. 1018899-04-1
Solubility (25°C)* 体外 DMSO 85 mg/mL (200.02 mM)
Ethanol 43 mg/mL warmed with 50ºC water bath (101.19 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 Sotagliflozin is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.
in vitro

LX4211 inhibits [14C]AMG uptake with IC50 of 62.0 nM for mouse SGLT1 and 0.6 nM for mouse SGLT2, respectively. [2]
in vivo

In mice, LX4211 (60 mg/kg, p.o.) reduces intestinal glucose absorption by inhibiting SGLT1, resulting in net increases in GLP-1 and PYY release and decreases in GIP release and blood glucose excursions. [2]

In nonobese diabetes-prone mice with type 1 diabetes, Sotagliflozin (30 mg/kg) significantly improves glycemic control, without increasing the rate of hypoglycemia measurements. [3]

プロトコル(参考用のみ)

キナーゼアッセイ In vitro Human SGLT2/SGLT1 Inhibition Assay
Human SGLT2 is cloned into pIRESpuro2 vector for mammalian expression (construct: HA-SGLT2-pIRESpuro2). HEK293 cells are transfected with the human HA-SGLT2-pIRESpuro2 vector and the stably transfected cell line is established in the presence of 0.5 μg/mL of puromycin. Human HA-SGLT2 cells are maintained in DMEM media containing 10% FBS, 1% GPS and 0.5 μg/mL of puromycin. The HEK293 cells expressing the human HA-SGLT2 are seeded in 384 well plates (30,000 cells/well) in DMEM media containing 10% FBS, 1% GPS and 0.5 μg/mL of puromycin, then incubated overnight at 37 C, 5% CO2. Cells are then washed with uptake buffer (140 mM NaCl, 2 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 10 mM HEPES, 5 mM Tris, 1 mg/mL bovine serum albumin (BSA), pH 7.3). Twenty microliters of uptake buffer with or without testing compounds are added to the cells. Then, 20 microliters of uptake buffer containing 14C-AMG (100 nCi) are added to the cells. The cell plates are incubated at 37°C, 5% CO2 for 1-2 hours. After washing the cells with uptake buffer, scintillation fluid is added (40 microliters/well) and 14C-AMG uptake is measured by counting radioactivity using a scintillation coulter. Human SGLT1 is cloned into pIRESpuro2 vector for mammalian expression (construct: HA-SGLT1-pIRESpuro2 ). HEK293 cells are transfected with the human HA-SGLT1-pIRESpuro2 vector and the stably transfected cell line is established in the presence of 0.5 μg/mL of puromycin. Human HA-SGLT1 cells are maintained in DMEM media containing 10% FBS, 1% GPS and 0.5 μg/mL of puromycin. The HEK293 cells expressing the human HA-SGLT1 were seeded in 384 well plates (30,000 cells/well) in DMEM media containing 10% FBS, 1% GPS and 0.5 μg/mL of puromycin, then incubated overnight at 37 C, 5% CO2. Cells were then washed with uptake buffer (140 mM NaCl, 2 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 10 mM HEPES, 5 mM Tris, 1 mg/mL bovine serum albumin (BSA), pH 7.3). Twenty microliters of uptake buffer with or without testing compounds are added to the cells. Then, 20 microliters of uptake buffer containing 14C-AMG (100 nCi) are also added to cells. The cell plates are incubated at 37°C, 5% CO2 for 1-2 hours. After washing the cells with uptake buffer, scintillation fluid is added (40 microliters/well) and 14C-AMG uptake was measured by counting radioactivity using a scintillation
細胞アッセイ 細胞株 Cell-free assays
濃度 36 nM (SGLT1) and 1.8 nM (SGLT2)
反応時間
実験の流れ
動物実験 動物モデル Male albino C57BL/6-Tyrc-Brd mice
投薬量 ~60 mg/kg
投与方法 p.o.

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：

Sucrose overconsumption impairs AgRP neuron dynamics and promotes palatable food intake [ Cell Rep, 2024, 43(2):113675] PubMed: 38224492
The impact of SGLT2 inhibitors on αKlotho in renal MDCK and HK-2 cells [ Front Endocrinol (Lausanne), 2023, 14:1069715] PubMed: 36967770
Sotatercept analog improves cardiopulmonary remodeling and pulmonary hypertension in experimental left heart failure [ Front Cardiovasc Med, 2023, 10:1064290] PubMed: 36910526
The sodium/glucose cotransporters as potential therapeutic targets for CF lung diseases revealed by human lung organoid swelling assay [ Mol Ther Methods Clin Dev, 2022, 24:11-19] PubMed: 34977268
SGLT2 promotes pancreatic cancer progression by activating the Hippo signaling pathway via the hnRNPK-YAP1 axis [ Cancer Lett, 2021, 519:277-288] PubMed: 34314754
Brown adipocyte ATF4 activation improves thermoregulation and systemic metabolism [ Cell Rep, 2021, 36(12):109742] PubMed: 34551310
Androgen Signaling Regulates SARS-CoV-2 Receptor Levels and Is Associated with Severe COVID-19 Symptoms in Men [ Cell Stem Cell, 2020, 27(6):876-889.e12] PubMed: 33232663
Leptin enhances glycolysis via OPA1-mediated mitochondrial fusion to promote mesenchymal stem cell survival [ Int J Mol Med, 2019, 44(1):301-312] PubMed: 31115489
Hyperglycaemic impairment of PAR2-mediated vasodilation: Prevention by inhibition of aortic endothelial sodium-glucose-co-Transporter-2 and minimizing oxidative stress [Xie C J Cell Mol Med, 2018, 22(11):5367-5377] PubMed: 30156363
Hyperglycaemic impairment of PAR2-mediated vasodilation: Prevention by inhibition of aortic endothelial sodium-glucose-co-Transporter-2 and minimizing oxidative stress. [ Vascul Pharmacol, 2018, 109:56-71] PubMed: 29908295

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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