LY2608204 - 10mM in DMSO , Hexokinase type IV activator, CAS No.1234703-40-2, Hexokinase type IV activator

CAS: 1234703-40-2 Cat. No.: L407980 Fórmula: C₂₈H₃₇N₃O₃S₃ Peso molecular: 559.81

GRADE & PURITY 10mM in DMSO

Synonyms

(1R,2S)-2-cyclohexyl-1-(4-(cyclopropylsulfonyl)phenyl)-N-(5-(2-(pyrrolidin-1-yl)ethylthio)thiazol-2-yl)cyclopropanecarboxamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

LY2608204 LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2.
In vitro

LY2608204 activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. LY2608204 also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM.

In vivo

LY2608204 decreases plasma glucose in a dose-dependent manner at both fasted and postprandial glucose levels. A maximal lowering of glucose AUC versus the untreated control group is observed with the high dose (30 mg/kg) and represents a 42% decrease. Interpolation of the data show that a 20% glucose AUC decrease occurs at an average LY2608204 concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg LY2608204 dose. The in vivo blood brain barrier permeability of LY2608204 results in a mean brain/plasma ratio of 0.17 five minutes post-dose with a mean total brain level of 0.539 nmol/g.
Cell Data

cell lines：Gpx4^−/−cells

Concentrations：

Incubation Time：

Powder Purity:≥97%

Specifications

Sinónimos

(1R,2S)-2-cyclohexyl-1-(4-(cyclopropylsulfonyl)phenyl)-N-(5-(2-(pyrrolidin-1-yl)ethylthio)thiazol-2-yl)cyclopropanecarboxamide

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2.

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.

Tipo de ação

ACTIVATOR

Mecanismo de ação

Hexokinase type IV activator

Propriedades do produto

• ALogP: 6.2

Nomes e identificadores

• SMILES isoméricas: C1CCC(CC1)[C@@H]2C[C@@]2(C3=CC=C(C=C3)S(=O)(=O)C4CC4)C(=O)NC5=NC=C(S5)SCCN6CCCC6
• Peso molecular: 559.81
• Reaxy-Rn: 20420503
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20420503&ln=

Propriedades químicas e físicas

• Solubilidade: Solubility (25°C) In vitro