|Description||GSK 962040 is a selective motilin receptor agonist with pEC50 value of 7.9. It is effective as a stimulant of human and rabbit gastrointestinal motility. lt represents a new opportunity as a treatment in diabetic gastroparesis. It is discovered as a therapeutic agent for conditions associated with delayed gastric emptying. It is highly selective against motilin receptor over the human ghrelin receptor and hERG. It also has no significant activity against other receptors including 5-HT, adrenergic, dopamine, histamine and adenosine receptors. It is found to enhance the EFS-induced cholinergic contraction and cause a small muscle contraction at high concentration in rabbit isolated gastric antrum. It also induces the contraction of human-isolated stomach preparations at 10μM. It had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes in vitro. It was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM. It induced phasic contractions, the duration of which was dose-related. It strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only. It was developed by glaxosmithkline and has been in Cilinic Phase 2.|
|Appearance||White to off-white Solid|
|Solubility||10 mM in DMSO|
|Application||GSK 962040 may be used as a treatment in diabetic gastroparesis.|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
|Boiling Point||610.0±55.0 °C | Condition: Press: 760 Torr|
|Melting Point||144 °C|
|Density||1.175±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr|
|Current Developer||GSK 962040 was developed by glaxosmithkline and has been in Cilinic Phase 2.|
GSK 962040 hydrochloride
GSK 962040 hydrochloride is the hydrochloride form of GSK 962040, which is a selective motilin receptor agonist with pEC50 value of 7.9. It may be used as a tre...
Motilin(human, porcine) is an endogenous motilin receptor ligand (Ki= 2.3 nM, and EC50= 0.3 nM in a Chinese hamster ovary cell line) that regulates gastrointest...
GSK 962040 is a selective motilin receptor agonist with pEC50 value of 7.9. It is effective as a stimulant of human and rabbit gastrointestinal motility. lt rep...