Sotagliflozin
Based on 12 publication(s) in Google Scholar
Sotagliflozin (LX-4211) is a potent dual SGLT2/1 inhibitor. Antidiabetic agents.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.94%
- CAS 番号: 1018899-04-1
- 分子式: C21H25ClO5S
- 分子量:424.94
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Sotagliflozin
More- Nat Cell Biol. 2021 Jul;23(7):733-744. [Abstract]
- Curr Biol. 2022 Apr 11;32(7):1485-1496.e4. [Abstract]
- Oncogene. 2021 Jul;40(29):4796-4808. [Abstract]
- Biochem Pharmacol. 2016 Feb 1:101:27-39. [Abstract]
- J Ethnopharmacol. 2021 Feb 10;266:113398. [Abstract]
- Int Immunopharmacol. 2025 Sep 1:165:115461. [Abstract]
- iScience. 2023 Jul 3;26(8):107260. [Abstract]
- J Nutr. 2020 Jul 1;150(7):1790-1798. [Abstract]
- Front Biosci-Landmrk. 2022, 27(12), 321.
- bioRxiv. 2025 May 19.
- Preprints. 2024 Jun 04.
- Preprints. 2024 Feb 8.
Customer Validation & Images
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WB
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2D/3D Cell Culture and Differentiation
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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生物活性
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SGLT1 |
SGLT2 |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
1.8 nM
Compound: 1
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Inhibition of human HA-tagged SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
Inhibition of human HA-tagged SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
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[PMID: 28045524] |
| HEK293 | IC50 |
36.2 nM
Compound: 1
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Inhibition of human HA-tagged SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
Inhibition of human HA-tagged SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
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[PMID: 28045524] |
LX4211 enhanced urinary glucose excretion by inhibiting SGLT2-mediated renal glucose reabsorption; markedly and significantly improved multiple measures of glycemic control, including fasting plasma glucose, oral glucose tolerance, and HbA(1c); and significantly lowered serum triglycerides. LX4211 also mediated trends for lower weight, lower blood pressure, and higher glucagon-like peptide-1 levels. In a follow-up single-dose study in 12 patients with T2DM, LX4211 (300 mg) significantly increased glucagon-like peptide-1 and peptide YY levels relative to pretreatment values, probably by delaying SGLT1-mediated intestinal glucose absorption [1]. LX4211-treated mice and SGLT1-/- mice also had increased GLP-1 AUC values, decreased glucose-dependent insulinotropic polypeptide (GIP) AUC values, and decreased blood glucose excursions during the 6 hours after a challenge with oral glucose alone [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1018899-04-1
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性状 Solid
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分子量 424.94
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分子式 C21H25ClO5S
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Color White to off-white
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SMILES
ClC(C=CC([C@@H]1O[C@H](SC)[C@@H](O)[C@H](O)[C@H]1O)=C2)=C2CC3=CC=C(OCC)C=C3
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別名
LX-4211; LP-802034
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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Nat Cell Biol
2021 Jul;23(7):733-744. PMID: 34155381
Sotagliflozin purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2021 Jul;23(7):733-744. [Abstract]
Representative images of Day 4 organoids from the Sotagliflozin-treated samples for SGLT-1 inhibition, with quantification of the eccentricity and lumen ratio (lumen volume vs. total volume) of control and Sotagliflozin-treated organoids from three independent experiments. Sotagliflozin (5 μM; 24 h) significantly impaired the reduction in lumen volume and crypt budding.
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Curr Biol
2022 Apr 11;32(7):1485-1496.e4. PMID: 35196509 -
Oncogene
2021 Jul;40(29):4796-4808. PMID: 34155348
Sotagliflozin purchased from MedChemExpress. Usage Cited in: Oncogene. 2021 Jul;40(29):4796-4808. [Abstract]
The effects of Phlorizin (100 μM) or LX4211 (Sotagliflozin; 1 μM; 3-day pretreatment, 4 h incubation, 37 °C 20 min ) on glucose uptake in H322/ER#1 and H322/ER#2 cells under a low-glucose condition were measured using a 2-NBDG assay. LX4211 reduced 2-NBDG uptake in H322/ER#1 and H322/ER#2 cells.
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J Ethnopharmacol
Inhibitory effects of Gymnema inodorum (Lour.) Decne leaf extracts and its triterpene saponin on carbohydrate digestion and intestinal glucose absorption. [Abstract]2021 Feb 10;266:113398. PMID: 32971162
Sotagliflozin purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2021 Feb 10;266:113398. [Abstract]
Inhibition of 2-NBDG uptake in Caco-2 cells after 30 min pretreatment with LX4211 (Sotagliflozin; 0.1 μg/mL), followed by measurement of 2-NBDG uptake. LX4211 time-dependently inhibited 2-NBDG uptake in Caco-2 cells, with inhibition increasing from approximately 40% at 5 min to nearly 90% at 30 min.
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Int Immunopharmacol
Sotagliflozin attenuates atrial oxidative stress and the susceptibility to atrial fibrillation by activating the NRF2/HO-1 pathway. [Abstract]2025 Sep 1:165:115461. PMID: 40897116
Sotagliflozin purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Sep 1:165:115461. [Abstract]
Western blot results of SERCA, NCX1, p-CAMKII, and CAMKII in HL-1 cells. Sota (Sotagliflozin; 10 μM; 1 h pretreatment; 24 h pacing) reversed the pacing-induced decrease in SERCA and increase in NCX1 and notably reduced p-CAMKII levels.
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iScience
SGLT1/2 inhibition improves glycemic control and multi-organ protection in type 1 diabetes. [Abstract]2023 Jul 3;26(8):107260. PMID: 37520739 -
J Nutr
Dietary Glucose Increases Glucose Absorption and Lipid Deposition via SGLT1/2 Signaling and Acetylated ChREBP in the Intestine and Isolated Intestinal Epithelial Cells of Yellow Catfish. [Abstract]2020 Jul 1;150(7):1790-1798. PMID: 32470978
Sotagliflozin purchased from MedChemExpress. Usage Cited in: J Nutr. 2020 Jul 1;150(7):1790-1798. [Abstract]
Effects of LX-4211 pretreatment on glucose-induced changes in protein expression in IECs of yellow catfish. Primary IECs are incubated in control or glucose (15 mM glucose) for 24 h with or without 2-h pretreatment with an SGLT1/2 dual inhibitor LX-4211 (20 μM).
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溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (235.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 50 mg/mL (117.66 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (274 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Zambrowicz B, et al. LX4211, a dual SGLT1/SGLT2 inhibitor, improved glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial. Clin Pharmacol Ther. 2012 Aug;92(2):158-69. [Content Brief]
[2]. Powell DR, et al. LX4211 increases serum glucagon-like peptide 1 and peptide YY levels by reducing sodium/glucose cotransporter 1 (SGLT1)-mediated absorption of intestinal glucose. J Pharmacol Exp Ther. 2013 May;345(2):250-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.3533 mL | 11.7664 mL | 23.5327 mL | 58.8318 mL |
| 5 mM | 0.4707 mL | 2.3533 mL | 4.7065 mL | 11.7664 mL | |
| 10 mM | 0.2353 mL | 1.1766 mL | 2.3533 mL | 5.8832 mL | |
| 15 mM | 0.1569 mL | 0.7844 mL | 1.5688 mL | 3.9221 mL | |
| 20 mM | 0.1177 mL | 0.5883 mL | 1.1766 mL | 2.9416 mL | |
| 25 mM | 0.0941 mL | 0.4707 mL | 0.9413 mL | 2.3533 mL | |
| 30 mM | 0.0784 mL | 0.3922 mL | 0.7844 mL | 1.9611 mL | |
| 40 mM | 0.0588 mL | 0.2942 mL | 0.5883 mL | 1.4708 mL | |
| 50 mM | 0.0471 mL | 0.2353 mL | 0.4707 mL | 1.1766 mL | |
| 60 mM | 0.0392 mL | 0.1961 mL | 0.3922 mL | 0.9805 mL | |
| 80 mM | 0.0294 mL | 0.1471 mL | 0.2942 mL | 0.7354 mL | |
| 100 mM | 0.0235 mL | 0.1177 mL | 0.2353 mL | 0.5883 mL |
Sotagliflozin 関連分類
HY-15516 関連分類
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