GHSR1a Agonist

Ibutamoren (MK-677 free base; MK-0677 free base) is an orally active non-peptide growth hormone secretagogue receptor agonist. Ibutamoren activates signal cascades by mimicking endogenous ligands, triggers pulsatile release of growth hormone from the pituitary gland, and increases serum levels of IGF-1 and insulin-like growth factor-binding protein 3. Ibutamoren not only increases the frequency of growth hormone pulses in male individuals, but also promotes elevated bone formation markers in female individuals with postmenopausal osteoporosis. The combination of Ibutamoren with Alendronate sodium hydrate (HY-11101) significantly increases bone mineral density at the femoral neck. However, Ibutamoren may cause mild, reversible adverse reactions such as increased appetite, fluid retention, and elevated fasting blood glucose. Ibutamoren has been widely used in studies related to idiopathic growth hormone deficiency, sarcopenia, Alzheimer's disease, and osteoporosis.

KARI 201 hydrochloride is an orally active, blood-brain barrier-penetrant bifunctional small molecule. KARI 201 hydrochloride is a selective inhibitor of ASM and an agonist of GHSR-1a. KARI 201 hydrochloride competitively binds ASM, inhibits ASM activity to reduce intracellular ceramide levels, restores lysosomal biogenesis, and repairs impaired autophagic flux in neurons. KARI 201 hydrochloride activates GHSR-1a and induces calcium influx. KARI 201 hydrochloride ameliorates Alzheimer's disease-related pathology, age-related sarcopenia phenotypes, and postoperative ileus-related symptoms. KARI 201 hydrochloride can be used in Alzheimer's disease-related research.

KARI 201 is an orally active, blood-brain barrier-penetrant bifunctional small molecule. KARI 201 is a selective inhibitor of ASM and an agonist of GHSR-1a. KARI 201 competitively binds ASM, inhibits ASM activity to reduce intracellular ceramide levels, restores lysosomal biogenesis, and repairs impaired autophagic flux in neurons. KARI 201 activates GHSR-1a and induces calcium influx. KARI 201 ameliorates Alzheimer's disease-related pathology, age-related sarcopenia phenotypes, and postoperative ileus-related symptoms. KARI 201 can be used in Alzheimer's disease-related research.

AZ-GHS-38 (compound 38) is an orally active CNS-penetrant inverse agonist of growth hormone secretagogue receptor (GHS-R1a) with an IC₅₀ of 6.7 nM. AZ-GHS-38 results in acute reduction of food intake in wild-type mice. AZ-GHS-38 can be used for anti-obesity research.

GHSR-1a agonist-1 (Compound 4b) is an orally active agonist of the human growth hormone secretagogue receptor 1a (GHSR-1a), with an EC₅₀ of 0.49 nM. GHSR-1a agonist-1 can effectively stimulate the release of endogenous growth hormone by activating GHSR-1a. GHSR-1a agonist-1 administered orally at a dose as low as 0.1 mg/kg can increase the body weight and body length of 4-week-old rats. GHSR-1a agonist-1 can be used in the research field of growth and development retardation in children.