bs-60209C

DATASHEET

Formulation powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 418.9

Formula: C18 H19 Cl N6 O2 S

CAS Number: 1621175-65-2

InChi Key: DRSZMILOMUPIBJ-UHFFFAOYSA-N

InChi: InChI=1S/C18H19ClN6O2S/c1-20-18-23-16(15-5-3-4-8-21-15)10-17(24-18)22-11-12-6-7-13(9-14(12)19)25-28(2,26)27/h3-10,25H,11H2,1-2H3,(H2,20,22,23,24)

Smiles: CNC1=NC(=CC(NCC2C=CC(=CC=2Cl)NS(C)(=O)=O)=N1)C1C=CC=CN=1

Purity: 98.0

Solubility: DMSO up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years

Description:

GPR39-C3 is the first potent, selective and orally bioavailable GPR39 agonist with an EC50 ~0.8 nM for human GPR39 and ~0.4 nM for rodent GPR39. It has no inhibitory effects (at 10 μM) on a panel of kinases and exhibits no relevant binding affinity for the related ghrelin and neurotensin-1 receptors and other enzymes, transporters, and GPCRs. GPR39-C3 has excellent functional activity in physiologically relevant rodent cells and in vivo. An acute study in normal mice with orally administrated GPR39-C3 confirmed in vitro findings by demonstrating an increase of the relevant pharmacodynamic marker GLP-1. It is a good chemical tool to enable interrogation of GPR39 signaling in different cellular contexts.