Empagliflozin (BI 10773) - Moligand™, 10mM in DMSO , Sodium/glucose cotransporter 2 inhibitor, CAS No.864070-44-0, Sodium/glucose cotransporter 2 inhibitor

CAS: 864070-44-0 Cat. No.: E409159 Fórmula: C₂₃H₂₇ClO₇ Peso molecular: 450.91 Número CE: 620-176-8

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

D-Glucitol, 1,5-anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl]methyl]phenyl]-, (1S)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

Empagliflozin (BI-10773) is a potent and selectiveSGLT-2inhibitor withIC50of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. Phase 3.
In vitro

Empagliflozin shows >2500-fold selectivity for hSGLT-2 over hSGLT-1 (IC50 8300 nM) and >3500-fold selectivity over hSGLT-4, it exhibits >350-fold selectivity over hSGLT-5 (IC50=1100 nM) and >600-fold selectivity over hSGLT-6. No relevant inhibition of GLUT1 is observed up to 10 μM Empagliflozin. In a kinetic binding experiments, [³H]-empagliflozin displays a high affinity for SGLT-2 with a mean K_d of 57 nM in the absence of glucose, and shows a half-life of [³H]-empagliflozin-binding to SGLT-2 of 59 min in the absence of glucose.Its binding to SGLT-2 is competitive with glucose.

In vivo

Cell Data

cell lines：

Concentrations：~ 500 nM

Incubation Time：72 h

Powder Purity:≥99%

Specifications

Sinónimos

D-Glucitol, 1,5-anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl]methyl]phenyl]-, (1S)-

Especificações e pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos e fisiológicos

Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. Phase 3.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Grau

Moligand™

Tipo de ação

INHIBITOR

Mecanismo de ação

Sodium/glucose cotransporter 2 inhibitor

Propriedades do produto

ALogP

2

Nomes e identificadores

SMILES isoméricas

C1COC[C@H]1OC2=CC=C(C=C2)CC3=C(C=CC(=C3)[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)Cl

CAS alternativo

864070-44-0

Termos de entrada MeSH

1-chloro-4-(glucopyranos-1-yl)-2-(4-(tetrahydrofuran-3-yloxy)benzyl)benzene;BI 10773;BI-10773;BI10773;empagliflozin;Jardiance

Peso molecular

450.91

Reaxy-Rn

31635249

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=31635249&ln=

Alvos associados (humanos)

SLC5A2 Tclin Sodium/glucose cotransporter 2 (5 Activities)

Discover Target: SLC5A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC5A1 Tclin Sodium/glucose cotransporter 1 (1 Activities)

Discover Target: SLC5A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propriedades químicas e físicas

• Solubilidade: Solubility (25°C) In vitro DMSO: 30 mg/mL (199.82 mM); Water: 30 mg/mL (199.82 mM); Ethanol: Insoluble