受注:045-509-1970 |
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Synonyms | LP-802034, LX4211 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C21H25ClO5S |
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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. |
製品説明 | Sotagliflozin is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3. |
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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] |
キナーゼアッセイ | In vitro Human SGLT2/SGLT1 Inhibition Assay | |
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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. |
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。
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。