LX-4211

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 SGLT2 抑制剂，对 hSGLT2 的 IC50 为 14 nM。

A potent, selective SGLT2 inhibitor with IC50 of 14 nM for hSGLT2; exhibits excellent selectivity over hSGLT1 (IC50=19 uM); inhibits SGLT2 in vitro and urinary glucose reabsorption in vivo.Diabetes Phase 2 Clinical(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 . 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.

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 . 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 .

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Sotagliflozin | LP-802034 | LX4211 | LX 4211

GPCR/G Protein

SGLT

SGLT1|SGLT2

Metabolic Disease

Diabetes

1018899-04-1

424.9382

C21H25ClO5S

>98% (HPLC)

10 mM in DMSO

O[C@@H]([C@@H]([C@H]([C@H](C1=CC=C(Cl)C(CC2=CC=C(OCC)C=C2)=C1)O3)O)O)[C@H]3SC

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

(-20℃)

With Ice Pack

≥ 2 years