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LX-4211

Names

[ CAS No. ]:
1018899-04-1

[ Name ]:
LX-4211

[Synonym ]:
sotagliflozin
LP-802034
(2S,3R,4R,5S,6R)-2-[4-chloro-3-(4-ethoxy-benzyl)-phenyl]-6-methylsulfanyl-tetrahydro-pyran-3,4,5-triol
β-L-Xylopyranoside, methyl 5-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-1-thio-, (5S)-
LX-4211
(2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(methylthio)tetrahydro-2H-pyran-3,4,5-triol
LX4211
CS-1069
LX 4211
Methyl (5S)-5-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1-thio-β-L-xylopyranoside
UNII-6B4ZBS263Y

Biological Activity

[Description]:

LX-4211 is a potent dual SGLT2/1 inhibitor; Antidiabetic agents.IC50 value:Target: SGLT1/2LX4211 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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> SGLT
Research Areas >> Metabolic Disease

[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.


[Related Small Molecules]

Phlorizin | Phloretin | Ertugliflozin | Licogliflozin | Tofogliflozin (hydrate) | Bexagliflozin | Ipragliflozin | Velagliflozin

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
607.9±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C21H25ClO5S

[ Molecular Weight ]:
424.938

[ Flash Point ]:
321.4±31.5 °C

[ Exact Mass ]:
424.111115

[ PSA ]:
104.45000

[ LogP ]:
5.63

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.642

[ Storage condition ]:
-20℃

Related Compounds