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LX-4211

SGLT1/SGLT2 inhibitor CAS# 1018899-04-1

LX-4211

Catalog No. BCC1714----Order now to get a substantial discount!

Product Name & Size Price Stock
LX-4211:5mg $105.00 In stock
LX-4211:10mg $179.00 In stock
LX-4211:25mg $420.00 In stock
LX-4211:50mg $735.00 In stock
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Quality Control of LX-4211

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Chemical structure

LX-4211

3D structure

Chemical Properties of LX-4211

Cas No. 1018899-04-1 SDF Download SDF
PubChem ID 24831714 Appearance Powder
Formula C21H25ClO5S M.Wt 424.94
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Sotagliflozin; LP-802034
Solubility DMSO : ≥ 100 mg/mL (235.33 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (2S,3R,4R,5S,6R)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-methylsulfanyloxane-3,4,5-triol
SMILES CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C3C(C(C(C(O3)SC)O)O)O)Cl
Standard InChIKey QKDRXGFQVGOQKS-CRSSMBPESA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of LX-4211

DescriptionLX-4211 is a potent dual SGLT2/1 inhibitor; Antidiabetic agents. IC50 value: Target: SGLT1/2 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].

References:
[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. [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.

LX-4211 Dilution Calculator

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LX-4211 Molarity Calculator

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Preparing Stock Solutions of LX-4211

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3533 mL 11.7664 mL 23.5327 mL 47.0655 mL 58.8318 mL
5 mM 0.4707 mL 2.3533 mL 4.7065 mL 9.4131 mL 11.7664 mL
10 mM 0.2353 mL 1.1766 mL 2.3533 mL 4.7065 mL 5.8832 mL
50 mM 0.0471 mL 0.2353 mL 0.4707 mL 0.9413 mL 1.1766 mL
100 mM 0.0235 mL 0.1177 mL 0.2353 mL 0.4707 mL 0.5883 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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The Institute of Cancer Research

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Universite de Paris
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The University of Tokyo
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Background on LX-4211

LX-4211 is a dual SGLT2/1 inhibitor; Antidiabetic agents.

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References on LX-4211

American Diabetes Association--70th scientific sessions--research on novel therapeutics: part 1.[Pubmed:20799136]

IDrugs. 2010 Sep;13(9):595-7.

The American Diabetes Association 70th Scientific Sessions, held in Orlando, FL, USA, included topics covering new therapeutic developments in the field of diabetes research. This conference report highlights selected presentations on new research with novel agents. Investigational drugs discussed include the glucagon-like peptide-1 (GLP-1) agonist taspoglutide (Roche Holding AG/Teijin Ltd/ Chugai Pharmaceutical Co Ltd), the GLP-1 analog SKL-18287 (Sanwa Kagaku Kenkyusho Co Ltd), the sodium glucose transporter-2 (SGLT2) inhibitor ASP-1941 (Astellas Pharma Inc/Kotobuki Pharmaceutical Co Ltd), the dual SGLT2/1 inhibitor LX-4211 (Lexicon Pharmaceuticals Inc), and the selective PPARgamma modulator INT-131 (InteKrin Therapeutics Inc).

Description

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

Keywords:

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