GPCR/G Protein GHSR Capromorelin Tartrate

Capromorelin Tartrate

Catalog No. TQ0022   CAS 193273-69-7
Synonyms: CP 424391-18

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

Capromorelin Tartrate, CAS 193273-69-7
Pack Size Availability Price/USD Quantity
2 mg In stock 50.00
5 mg In stock 72.00
10 mg In stock 132.00
25 mg In stock 285.00
50 mg In stock 492.00
100 mg In stock 779.00
1 mL * 10 mM (in DMSO) In stock 143.00
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Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Capromorelin Tartrate is a potent, orally active growth hormone secretagogue receptor (GHSR) agonist (Ki: 7 nM for hGHS-R1a).
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 μg membrane per well in 50 mM HEPES, pH 7.4, 10 mM MgCl2, 0.2% bovine serum albumin and the following protease inhibitors: 100 μg/mL bacitracin, 100 μg/mL benzamidine, 5 μg/mL aprotinin, 5 μg/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].
Animal Research
The study tested capromorelin flavored oral solution with 30 mg/mL of capromorelin compared to a matched placebo flavored oral solution treatment (which contains all the ingredients of the formulation without capromorelin) administered for 4 days. Dogs are randomized into two groups, with Group 1 receiving placebo (0.1 mL/kg) and Group 2 receiving 3.0 mg/kg. Both groups are treated once a day at approximately 9 AM each day. The first day of dosing is considered Day 0. The placebo and test drug are administered by a syringe placed in the corner of the mouth. The Day 0 weight is used for dose calculations [2].
Synonyms CP 424391-18
Purity 98.00%
Molecular Weight 655.7
Formula C32H40N5O10
CAS No. 193273-69-7


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

Solubility Information

DMSO: 100 mg/mL (152.51 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )


References and Literature
1. Carpino PA, et al. Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. Bioorg Med Chem. 2003 Feb 20;11(4):581-90. 2. 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.

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