[CAS NO. 1018899-04-1] Sotagliflozin

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PRODUCTS SPECIFICATIONS [1018899-04-1]

Catalog

HY-15516

Brand

MCE

CAS

1018899-04-1

DESCRIPTION [1018899-04-1]

Overview

MDL	MFCD22493506
Molecular Weight	424.94
Molecular Formula	C21H25ClO5S
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

For research use only. We do not sell to patients.

8 Publications Citing Use of MCE

Summary

Sotagliflozin (LX-4211) is a potent dual SGLT2/1 inhibitor. Antidiabetic agents.

IC50 & Target

SGLT1/2

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03063580	Sanofi	Diabetes Mellitus	February 27, 2017	Phase 1
NCT01916850	Lexicon Pharmaceuticals	Healthy	August 2013	Phase 1
NCT03242018	Lexicon Pharmaceuticals\|Sanofi	Type 2 Diabetes Mellitus\|Chronic Kidney Disease Stage 4	August 16, 2017	Phase 3
NCT02383940	Lexicon Pharmaceuticals\|Juvenile Diabetes Research Foundation\|Sanofi	Type 1 Diabetes Mellitus	April 2015	Phase 2
NCT02647918	Lexicon Pharmaceuticals	Renal Impairment\|Healthy	December 2015	Phase 1
NCT02531035	Lexicon Pharmaceuticals\|Sanofi	Type 1 Diabetes Mellitus (T1DM)\|High Level of Sugar (Glucose) in the Blood	September 2015	Phase 3
NCT02940379	Sanofi	Type 2 Diabetes Mellitus	October 2016	Phase 1
NCT03211195	Sanofi	Type 2 Diabetes Mellitus	June 29, 2017	Phase 1
NCT01441232	Lexicon Pharmaceuticals	Type 2 Diabetes Mellitus	October 2011	Phase 1
NCT02300350	Lexicon Pharmaceuticals	Healthy	October 2014	Phase 1
NCT02926937	Lexicon Pharmaceuticals\|Sanofi	Type 2 Diabetes Mellitus	November 11, 2016	Phase 3
NCT02926950	Lexicon Pharmaceuticals\|Sanofi	Type 2 Diabetes Mellitus	November 2016	Phase 3
NCT03315143	Lexicon Pharmaceuticals\|Sanofi	Heart Failure\|Type 2 Diabetes Mellitus\|Chronic Kidney Diseases	December 19, 2017	Phase 3
NCT03760965	Sanofi	Type 2 Diabetes Mellitus	November 27, 2018	Phase 3
NCT03462069	Sanofi	Diabetes Mellitus	March 12, 2018	Phase 2
NCT03802487	Sanofi	Type 2 Diabetes Mellitus\|Healthy Subjects	January 14, 2019	Phase 1
NCT03386344	Lexicon Pharmaceuticals\|Sanofi	Type 2 Diabetes Mellitus	February 19, 2018	Phase 3
NCT03387657	Sanofi	Type 2 Diabetes Mellitus	January 3, 2018	Phase 1
NCT02421510	Lexicon Pharmaceuticals\|Sanofi	Type 1 Diabetes Mellitus	May 2015	Phase 3
NCT03414723	Sanofi	Diabetes Mellitus\|Healthy Subjects	January 15, 2018	Phase 1
NCT03070678	Sanofi	Diabetes Mellitus	March 14, 2017	Phase 1
NCT02494609	Lexicon Pharmaceuticals	Healthy	July 2015	Phase 1
NCT02373046	Lexicon Pharmaceuticals	Healthy	February 2015	Phase 1
NCT05562063	Juan Badimon\|Icahn School of Medicine at Mount Sinai	Heart Failure With Preserved Ejection Fraction	October 26, 2022	Phase 4
NCT03292653	Lexicon Pharmaceuticals\|Sanofi	Cardiac Failure Aggravated	December 4, 2017	Phase 2
NCT03521934	Lexicon Pharmaceuticals\|Sanofi	Heart Failure\|Type 2 Diabetes Mellitus	June 15, 2018	Phase 3
NCT03242252	Lexicon Pharmaceuticals\|Sanofi	Type 2 Diabetes Mellitus\|Chronic Kidney Disease Stage 3	August 16, 2017	Phase 3
NCT01376557	Lexicon Pharmaceuticals	Type 2 Diabetes Mellitus	June 2011	Phase 2
NCT03285594	Lexicon Pharmaceuticals\|Sanofi	Type 2 Diabetes Mellitus	September 15, 2017	Phase 3
NCT03332771	Lexicon Pharmaceuticals\|Sanofi	Type 2 Diabetes Mellitus	December 1, 2017	Phase 3
NCT01916863	Lexicon Pharmaceuticals	Healthy Subjects	August 2013	Phase 1
NCT00962065	Lexicon Pharmaceuticals	Type 2 Diabetes Mellitus	August 2009	Phase 2
NCT03174548	Sanofi	Diabetes Mellitus	June 12, 2017	Phase 1
NCT03909451	Sanofi	Diabetes Mellitus	April 28, 2019	Phase 1
NCT02300363	Lexicon Pharmaceuticals	Healthy	October 2014	Phase 1
NCT02384941	Lexicon Pharmaceuticals\|Sanofi	Type 1 Diabetes Mellitus	March 2015	Phase 3
NCT01555008	Lexicon Pharmaceuticals	Type 2 Diabetes Mellitus\|Renal Impairment	March 2012	Phase 1
NCT03066830	Lexicon Pharmaceuticals\|Sanofi	Type 2 Diabetes Mellitus	February 24, 2017	Phase 3
NCT01188863	Lexicon Pharmaceuticals	Type 2 Diabetes Mellitus	September 2010	Phase 1
NCT02471274	Lexicon Pharmaceuticals	Hepatic Impairment\|Healthy	June 2015	Phase 1
NCT03776227	Sanofi	Type 2 Diabetes Mellitus\|Healthy Subjects	January 25, 2019	Phase 1
NCT03761134	Sanofi	Type 2 Diabetes Mellitus	November 30, 2018	Phase 3
NCT01913002	Lexicon Pharmaceuticals	Healthy	July 2013	Phase 1
NCT01292993	Lexicon Pharmaceuticals	Type 2 Diabetes Mellitus	February 2011	Phase 1
NCT01742208	Lexicon Pharmaceuticals\|Sanofi	Type 1 Diabetes Mellitus	February 2013	Phase 2
NCT02459899	Lexicon Pharmaceuticals\|Sanofi	Type 1 Diabetes Mellitus	July 2015	Phase 2
NCT03310944	Sanofi	Type 1 Diabetes Mellitus\|Type 2 Diabetes Mellitus	October 18, 2017	Phase 1
NCT03351478	Lexicon Pharmaceuticals\|Sanofi	Type 2 Diabetes Mellitus	November 27, 2017	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 235.33 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

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
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

β-L-Xylopyranoside, methyl 5-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-1-thio-, (5S)-

(5S)-Methyl 5-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-1-thio-β-L-xylopyranoside

Sotagliflozin

LP 802034

LX 4211

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