Sotagliflozin

Catalog No.S8103 Batch:S810301

Technical Data

Formula	C₂₁H₂₅ClO₅S
Molecular Weight	424.94	CAS No.	1018899-04-1
Solubility (25°C)*	In vitro	DMSO	84 mg/mL (197.67 mM)
		Ethanol	17 mg/mL (40.0 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Sotagliflozin is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.

Targets

SGLT2 ^[1]	SGLT1 ^[1]
1.8 nM	36 nM

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]

Protocol (from reference)

Kinase Assay:^{^[1]}	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
Animal Study:^{^[2]}	Animal Models Male albino C57BL/6-Tyrc-Brd mice Dosages ~60 mg/kg Administration p.o.

Kinase Assay:^{^[1]}

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

Animal Study:^{^[2]}

Animal Models
Male albino C57BL/6-Tyrc-Brd mice
Dosages
~60 mg/kg
Administration
p.o.

References

Selleck's Sotagliflozin has been cited by 10 publications

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

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