Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.
CAS：193273-69-7
分子式：C32H41N5O10
分子量：655.7
纯度：98%
存储：Store at -20°C

Background:

Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.

Capromorelin stimulates GH release in rat pituitary cell cultures with EC50 of 3 nM[2].

Dogs receiving capromorelin (30 mg/mL) have food consumption that is significantly greater than dogs treated with placebo. All dogs in the capromorelin group gain weight by 0.52 kg, more than that of placebo group[1]. Capromorelin shows enhanced intestinal absorption in rodent models and exhibits superior pharmacokinetic properties, including high bioavailabilities in two animal species [F(rat)=65%, F(dog)=44%][2]. Capromorelin stimulates GH release in anesthesized rat model, with ED50 of 0.05 mg/kg iv[2].

参考文献:
[1]. Zollers B, et al. Capromorelin oral solution (ENTYCE®) increases food consumption and body weight when administered for 4 consecutive days to healthy adult Beagle dogs in a randomized, masked, placebo controlled study. BMC Vet Res. 2017 Jan 5;13(1):10.
[2]. Carpino PA, et al. Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. Bioorg Med Chem. 2003 Feb 20;11(4):581-90.