Capromorelin Tartrate Inhibitor

Solid. Powder

98.98%

0-4 degree c for short term (days to weeks), or -20 degree c for long term (months).

655.7

DMSO: 100mg/mL (152.51mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

C32H40N5O10

O=C([C@@H]([C@@H](O)C(O)=O)O)O.CC(C)(N)C(N[C@](COCC1=CC=CC=C1)C(N(C[C@]23CC4=CC=CC=C4)CCC2=NN(C)C3=O)=O)=O

193273-69-7

In vitro:
Capromorelin stimulates GH release in rat pituitary cell cultures (EC50: 3 nM) [1].

In vivo:
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%][1]. Capromorelin stimulates GH release in the anesthesized rat model (ED50: 0.05 mg/kg iv) [1]. 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 the placebo group [2].

Kinase Assay:
Membranes are prepared from HEK293 cells stably transfected with the human GHS-R1a receptor cDNA in the plasmid pcDNA3.1neo. Competition radioligand binding assays are performed in 96-well format with GF/C filters pre-soaked in 0.3% polyethyleneimine. Assays are performed at room temperature for 1 h in duplicate using 50 pM [125I]-ghrelin and 1 ug membrane per well in 50 mM HEPES, pH 7.4, 10 mM MgCl2, 0.2% bovine serum albumin and the following protease inhibitors: 100 ug/mL bacitracin, 100 ug/mL benzamidine, 5 ug/mL aprotinin, 5 ug/mL leupeptin. The membranes are harvested and washed three times with ice-cold ish buffer containing 50 mM HEPES, pH 7.4 and 10 mM MgCl2. IC50 and Ki values are determined using Prism. The Kd of [125I]-ghrelin at membranes expressing human GHS receptors is calculated to be 0.2 nM [1].

GPCR/G Protein; GHSR