Sotagliflozin (LX4211)

Alias: Zynquista; LP-80203; LX4211; LP 80203; LX-4211; LP80203; LX 4211
Cat No.:V1501 Purity: ≥98%
Sotagliflozin (formerly known as LP-80203; LX4211; LP80203; LX-4211; Zynquista), an antidiabetic drug approved for treating type 1 diabetes in EU, is a potent, orally bioavailable, and dual SGLT1/SGLT2 inhibitor with antidiabetic activity.
Sotagliflozin (LX4211) Chemical Structure CAS No.: 1018899-04-1
Product category: SGLT
This product is for research use only, not for human use. We do not sell to patients.
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InvivoChem's Sotagliflozin (LX4211) has been cited by 1 publication
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Sotagliflozin (formerly known as LP-80203; LX4211; LP80203; LX-4211; Zynquista; Inpefa), an antidiabetic drug approved for treating type 1 diabetes in EU, is a potent, orally bioavailable, and dual SGLT1/SGLT2 inhibitor with antidiabetic activity. It blocks SGLT1/SGLT2 with IC50s of 36 nM and 1.8 nM, respectively. In a randomized, placebo-controlled study, sotagliflozin helps patients with type 2 diabetes achieve better glycemic control. By inhibiting the intestinal glucose absorption mediated by sodium/glucose cotransporter 1 (SGLT1), sotagliflozin also raises serum levels of peptide YY and glucagon-like peptide 1. Sotagliflozin (Inpefa) was approved in 2023 by FDA for treating Heart failure.

Biological Activity I Assay Protocols (From Reference)
Targets
SGLT1/2
ln Vitro

In vitro activity: LX4211 markedly and significantly improved multiple measures of glycemic control, including fasting plasma glucose, oral glucose tolerance, and HbA(1c); it also significantly decreased serum triglycerides and enhanced urine glucose excretion by inhibiting SGLT2-mediated renal glucose reabsorption. Additionally, LX4211 mediated trends toward decreased blood pressure, weight loss, and increased levels of glucagon-like peptide-1. LX4211 (300 mg) considerably raised glucagon-like peptide-1 and peptide YY levels in comparison to pretreatment values in a follow-up single-dose study involving 12 T2DM patients [1]. This effect was likely caused by delaying SGLT1-mediated intestinal glucose absorption. During the six hours following an oral glucose challenge, mice treated with LX4211 and SGLT1-/- mice likewise exhibited higher GLP-1 AUC values, lower glucose-dependent insulinotropic polypeptide (GIP) AUC values, and reduced blood glucose excursions[2].

ln Vivo
LX4211 (60 mg/kg, p.o.) inhibits SGLT1, which lowers intestinal glucose absorption in mice by increasing net GLP-1 and PYY release and decreasing GIP release and blood glucose excursions. Sotagliflozin (30 mg/kg) considerably enhances glycemic control in nonobese diabetes-prone mice with type 1 diabetes, without raising the frequency of hypoglycemia readings.
Animal Protocol
Dissolved in aqueous 0.1% v/v Tween 80; 60 mg/kg; oral administration.
Male albino C57BL/6-Tyrc-Brd mice
References

[1]. 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.

[2]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H25CLO5S
Molecular Weight
424.94
Exact Mass
424.11
Elemental Analysis
C, 59.36; H, 5.93; Cl, 8.34; O, 18.83; S, 7.55
CAS #
1018899-04-1
Appearance
White to off-white solid powder
SMILES
CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)SC)O)O)O)Cl
InChi Key
QKDRXGFQVGOQKS-CRSSMBPESA-N
InChi Code
InChI=1S/C21H25ClO5S/c1-3-26-15-7-4-12(5-8-15)10-14-11-13(6-9-16(14)22)20-18(24)17(23)19(25)21(27-20)28-2/h4-9,11,17-21,23-25H,3,10H2,1-2H3/t17-,18-,19+,20+,21-/m1/s1
Chemical Name
(2S,3R,4R,5S,6R)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-methylsulfanyloxane-3,4,5-triol
Synonyms
Zynquista; LP-80203; LX4211; LP 80203; LX-4211; LP80203; LX 4211
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~84 mg/mL (~197.7 mM)
Water: <1 mg/mL
Ethanol: ~17 mg/mL (~40.0 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3533 mL 11.7664 mL 23.5327 mL
5 mM 0.4707 mL 2.3533 mL 4.7065 mL
10 mM 0.2353 mL 1.1766 mL 2.3533 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05405556 Recruiting Diagnostic Test: eGFR reporting Kidney Transplant Martina McGrath, MD October 17, 2022 Phase 2
NCT05562063 Recruiting Drug: Sotagliflozin
Drug: Placebo
Heart Failure With Preserved
Ejection Fraction
Juan Badimon October 26, 2022 Phase 4
NCT06217302 Not yet recruiting Drug: Sotagliflozin
Drug: Placebo
Diabetic Nephropathies
Kidney Failure, Chronic
Alessandro Doria May 2024 Phase 3
NCT06147232 Not yet recruiting Drug: Sotagliflozin
Drug: Placebo
Nephropathy
Albuminuria
Steno Diabetes Center
Copenhagen
February 2024 Phase 4
NCT05696366 Not yet recruiting Drug: Sotagliflozin
Drug: Volagidemab
Type 1 Diabetes University of California,
San Diego
February 2023 Phase 1
Phase 2
Biological Data
  • Sotagliflozin (LX4211)
    Sotagliflozin significantly lowered blood glucose levels in mice with poorly controlled type 1 diabetes. Diabetes Metab Syndr Obes. 2015 Feb 26;8:121-7.
  • Sotagliflozin (LX4211)
    Sotagliflozin slowed the rise in A1c in mice with poorly controlled type 1 diabetes. Diabetes Metab Syndr Obes. 2015 Feb 26;8:121-7.
  • Sotagliflozin (LX4211)
    Insulin and β-hydroxybutyrate levels. Diabetes Metab Syndr Obes. 2015 Feb 26;8:
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