1.Description
Ibutamoren mesylate (MK-0677) is an orally active nonpeptide growth hormone (GH) secretagogue.
IC50 Value:
Target: GHSR
Ibutamoren mesylate (MK-0677) stimulates GH release through a pituitary and hypothalamic receptor that is different from the GH-releasing hormone receptor. MK-677is a drug which acts as a potent, orally active growth hormone secretagogue, mimicking the GH stimulating action of the endogenous hormone ghrelin. It has been demonstrated to increase the release of, and produces sustained increases in plasma levels of several hormones including growth hormone and IGF-1, but without affecting cortisol levels. It is currently under development as a potential treatment for reduced levels of these hormones, such as in growth hormone deficient children or elderly adults, and human studies have shown it to increase both muscle mass and bone mineral density, making it a promising therapy for the treatment of frailty in the elderly. Ibutamoren mesylate (MK-0677) also alters metabolism of body fat and so may have application in the treatment of obesity.
2 . Application area
An experimental drug meant to control lipids and increase the level of HDL, or good cholesterol, in the bloodstream. A cell-permeable, thiazolyl compound that acts as a potent, high affinity, PPARd agonist. Exhibits selectivity for PPARd compared t
Usage An experimental drug meant to control lipids and increase the level of HDL, or good cholesterol, in the bloodstream. A cell-permeable, thiazolyl compound that acts as a potent, high affinity, PPARδ agonist. Exhibits selectivity for PPARδ compared to PPARα and PPARγ. Does not exibit any activity against other nuclear or non-nuclear receptors. Reported to increase cholesterol efflux and ABAC1 expression in macrophages, fibroblasts, and intestinal cells.
3 . Specification:
TEST |
ACCEPTANCE CRITERLA |
RESULTS |
|
TLC |
Positive |
Identification |
UV spectrum |
Positive |
|
IR spectrum |
Positive |
Characteristics |
White to yellowish-white crystalline powder |
conform |
Melting point |
32 ~ 37ºC |
33~36ºC |
Specific optical rotation |
+77°~+82° |
+79.3° |
Loss on drying |
≤0.5% |
0.15% |
Assay |
97 ~ 103% |
99.08% |
Free heptanoic acid |
≤0.2 % |
0.10% |
Related substances |
≤2% |
Pass |
|
Acetone ≤100ppm |
Pass |
Residual solvents(GC) |
Methanol ≤100ppm |
Pass |
|
Pyridine ≤100ppm |
Pass |
Particle size |
|
Pass |