Globalagliatin

• CAT Number: I000935
• CAS Number: 1234703-40-2
• Molecular Formula: C28H37N3O3S3
• Molecular Weight: 559.81
• Purity: ≥95%
• Synonyms: (1R,2S)-2-cyclohexyl-1-(4-cyclopropylsulfonylphenyl)-N-[5-(2-pyrrolidin-1-ylethylsulfanyl)-1,3-thiazol-2-yl]cyclopropane-1-carboxamide
• InChI: InChI=1S/C28H37N3O3S3/c32-26(30-27-29-19-25(36-27)35-17-16-31-14-4-5-15-31)28(18-24(28)20-6-2-1-3-7-20)21-8-10-22(11-9-21)37(33,34)23-12-13-23/h8-11,19-20,23-24H,1-7,12-18H2,(H,29,30,32)/t24-,28-/m0/s1
• InChIKey: QIIVJLHCZUTGSD-CUBQBAPOSA-N
• SMILES: C1CCC(CC1)C2CC2(C3=CC=C(C=C3)S(=O)(=O)C4CC4)C(=O)NC5=NC=C(S5)SCCN6CCCC6

Globalagliatin (LY2608204) is a activator of glucokinase (GK) with EC50 of 42 nM.
IC 50 value: 42 nM (EC50)
Target: glucokinase
in vitro: Globalagliatin activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. Globalagliatin also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM.
in vivo: Globalagliatin 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 Globalagliatin concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg Globalagliatin dose. The in vivo blood brain barrier permeability of Globalagliatin 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.