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Capromorelin Tartrate

Capromorelin Tartrate
Capromorelin Tartrate (CP 424391-18) is a potent, orally active growth hormone secretagogue receptor (GHSR) agonist (Ki: 7 nM for hGHS-R1a).
Catalog No. TQ0022Cas No. 193273-69-7
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Purity:97.69%
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Capromorelin Tartrate

Catalog No. TQ0022Cas No. 193273-69-7

Capromorelin Tartrate (CP 424391-18) is a potent, orally active growth hormone secretagogue receptor (GHSR) agonist (Ki: 7 nM for hGHS-R1a).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
5 mg$33In Stock
10 mg$58In Stock
25 mg$128In Stock
50 mg$226In Stock
100 mg$335In Stock
200 mg$479In Stock
1 mL x 10 mM (in DMSO)$48In Stock
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Product Introduction

Bioactivity
Description
Capromorelin Tartrate (CP 424391-18) is a potent, orally active growth hormone secretagogue receptor (GHSR) agonist (Ki: 7 nM for hGHS-R1a).
Targets&IC50
GHS-R1a (human):7 nM (Ki)
In vitro
Capromorelin stimulates GH release in rat pituitary cell cultures (EC50: 3 nM) [1].
In vivo
Capromorelin demonstrates enhanced intestinal absorption in rodent models and exhibits superior pharmacokinetic properties, including high bioavailabilities in rats (F=65%) and dogs (F=44%) [1]. It stimulates GH release in anesthetized rats with an ED50 of 0.05 mg/kg iv [1]. In dogs, capromorelin (30 mg/mL) significantly increases food consumption and results in a weight gain of 0.52 kg compared to 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].
AliasCP 424391-18
Chemical Properties
Molecular Weight655.7
FormulaC32H41N5O10
Cas No.193273-69-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (152.51 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.5251 mL7.6254 mL15.2509 mL76.2544 mL
5 mM0.3050 mL1.5251 mL3.0502 mL15.2509 mL
10 mM0.1525 mL0.7625 mL1.5251 mL7.6254 mL
20 mM0.0763 mL0.3813 mL0.7625 mL3.8127 mL
50 mM0.0305 mL0.1525 mL0.3050 mL1.5251 mL
100 mM0.0153 mL0.0763 mL0.1525 mL0.7625 mL

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