[CAS NO. 1234703-40-2] LY2608204

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PRODUCTS SPECIFICATIONS [1234703-40-2]

Catalog

SLK-S2155

Brand

Selleck

CAS

1234703-40-2

DESCRIPTION [1234703-40-2]

Overview

MDL	MFCD21609257
Molecular Weight	559.81
Molecular Formula	C28H37N3O3S3
SMILES	O=C([C@@]1(C2=CC=C(S(=O)(C3CC3)=O)C=C2)[C@H](C4CCCCC4)C1)NC5=NC=C(SCCN6CCCC6)S5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.7863 mL	8.9316 mL	17.8632 mL
5 mM	0.3573 mL	1.7863 mL	3.5726 mL
10 mM	0.1786 mL	0.8932 mL	1.7863 mL
50 mM	0.0357 mL	0.1786 mL	0.3573 mL

Description

LY2608204 activates with of 42 nM. Phase 2.

Targets

glucokinase ^[1]

42 nM(EC50)

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.