"目录号: HY-15243
GPCR/G Protein-
Capromorelin Tartrate 是一种可口服的，有效的growth hormone secretagogue receptor (GHSR)激动剂，对hGHS-R1a的Ki值为 7 nM。
GHSR
相关产品
Anamorelin-Ibutamoren Mesylate-Alexamorelin-AZP-531-GHRP-2 metabolite 1-Examorelin-TC-G-1008-
生物活性
Description
Capromorelin Tartrate is an orally active, potentgrowth hormone secretagogue receptor (GHSR)agonist, withKiof 7 nM for hGHS-R1a.
IC50& Target
Ki: 7 nM (hGHS-R1a)[2]
In Vitro
Capromorelin stimulates GH release in rat pituitary cell cultures with EC50of 3 nM[2].
In Vivo
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 ED50of 0.05 mg/kg iv[2].
References
[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.